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ChEMBL ligand: CHEMBL54 (Dolpin, Dozic, Fortunan, Haldol, Haldol solutab, Haloperidol, Haloperidol decanoate impurity, haloperidol-, Kentace, Keselen, MCN-JR-1625, NSC-170973, NSC-615296, R-1625, Serenace) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125] | ||||||||
ChEMBL | Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 7.96 | pKi | 11 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
ChEMBL | Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta | B | 7.76 | pKd | 17.38 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418] |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.55 | pKi | 28 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.17 | pIC50 | 68 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.31 | pKi | 4.95 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.05 | pIC50 | 8.94 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.39 | pKi | 41 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.08 | pIC50 | 84 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.73 | pKi | 1865 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.3 | pIC50 | 4973 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.21 | pKi | 618 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.87 | pIC50 | 1354 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.57 | pKi | 268 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.73 | pIC50 | 1845 | nM | IC50 | DrugMatrix in vitro pharmacology data |
AP-2 complex subunit sigma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697667] [UniProtKB: P62744] | ||||||||
ChEMBL | Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting | B | 7.62 | pKi | 24.2 | nM | Ki | J Med Chem (2011) 54: 1555-1564 [PMID:21348515] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
ChEMBL | Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1986) 29: 1628-1637 [PMID:2875184] |
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] | ||||||||
ChEMBL | Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1986) 29: 1628-1637 [PMID:2875184] |
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352] | ||||||||
ChEMBL | Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Binding affinity towards human Dopamine receptor D1 | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | Binding affinity to human cloned dopamine D1 receptor | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Inhibition of human dopamine D1 receptor | B | 6.97 | pKi | 107 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Binding affinity for human recombinant dopamine receptor D1 | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (2004) 47: 4155-4158 [PMID:15293986] |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 7.26 | pKi | 55 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
GtoPdb | - | - | 8.2 | pKi | - | - | - |
Nature (1991) 350: 614-9 [PMID:1826762]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor | B | 8.21 | pKi | 6.17 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.96 | pIC50 | 110 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
ChEMBL | Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates | B | 7.03 | pKi | 93 | nM | Ki | J Med Chem (2011) 54: 4896-4903 [PMID:21599022] |
ChEMBL | Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane | B | 7.03 | pKi | 93 | nM | Ki | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
ChEMBL | Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay | B | 8.02 | pKi | 9.5 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579] |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand | B | 6.33 | pKi | 467 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
ChEMBL | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | B | 6.44 | pKi | 359 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method | B | 6.5 | pKi | 318 | nM | Ki | J Med Chem (2018) 61: 372-384 [PMID:29220177] |
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 6.5 | pKi | 318 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | B | 6.5 | pKi | 318 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor | B | 6.5 | pKi | 318 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand | B | 6.5 | pKi | 318 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | In vitro affinity against Dopamine receptor D1 | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane. | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding. | B | 6.84 | pKi | 145 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1 | B | 7.01 | pKi | 97.72 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 579-584 |
ChEMBL | Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1 | B | 7.01 | pKi | 97.72 | nM | Ki | J Med Chem (1991) 34: 2242-2247 [PMID:1676759] |
ChEMBL | Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane | B | 7.01 | pKi | 97.72 | nM | Ki | J Med Chem (1994) 37: 2564-2573 [PMID:7914540] |
ChEMBL | In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue | B | 7.12 | pKi | 76 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
ChEMBL | Binding affinity against dopamine receptor D1 | B | 7.12 | pKi | 75.86 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand. | B | 7.15 | pKi | 70.79 | nM | Ki | J Med Chem (2000) 43: 599-608 [PMID:10691686] |
ChEMBL | Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain | B | 7.24 | pKi | 58.08 | nM | Ki | Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521] |
ChEMBL | Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
ChEMBL | Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
ChEMBL | Binding affinity towards Dopamine receptor D1 | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
ChEMBL | Affinity for Dopamine receptor D1 | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525] |
ChEMBL | Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity | F | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (1987) 30: 1906-1910 [PMID:2888899] |
ChEMBL | Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand | B | 6.47 | pIC50 | 337 | nM | IC50 | J Med Chem (1991) 34: 3360-3365 [PMID:1662725] |
ChEMBL | Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
Dopamine D2 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5456] [UniProtKB: P52702] | ||||||||
ChEMBL | Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1995) 38: 4950-4952 [PMID:8523409] |
ChEMBL | Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2 | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1995) 38: 2251-2255 [PMID:7783157] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay | B | 9.31 | pKd | 0.49 | nM | Kd | J Med Chem (2019) 62: 9488-9520 [PMID:31580666] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopaminergic D2 receptor expressed in rat C6 cells | B | 5.19 | pKi | 6400 | nM | Ki | J Med Chem (2008) 51: 7602-7613 [PMID:19053888] |
ChEMBL | Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand | B | 6.66 | pKi | >217 | nM | Ki | J Med Chem (1994) 37: 2735-2753 [PMID:8064801] |
ChEMBL | Displacement of the radioligand [3H]spiperone from the cloned human Dopamine receptor D2 long expressed in CHO cells | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay | B | 8.02 | pKi | 9.6 | nM | Ki | Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D2 in CHO cells | F | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.2 | pKi | 6.33 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | B | 8.21 | pKi | 6.22 | nM | Ki | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | B | 8.21 | pKi | 6.17 | nM | Ki | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
ChEMBL | Displacement of [3H]methylspiperonee from recombinant human D2 receptor expressed in HEK293 cells cell membranes after 60 mins by liquid scintillation counting method | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression. | B | 8.25 | pKi | 5.6 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
ChEMBL | Displacement of [3H]-N-Methylspiperone from human dopamine D2 receptor expressed in stable fibroblast cells incubated for 90 mins by microbeta counting method | B | 8.25 | pKi | 5.58 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Displacement of [3H]N-methylspiperone from dopamine D2 receptor (unknown origin) | B | 8.25 | pKi | 5.58 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127305-127305 [PMID:32631525] |
ChEMBL | Displacement of [3H]YM-09151-2 from human dopamine D2S receptor in membrane suspensions by liquid scintillation counter | B | 8.29 | pKi | 5.09 | nM | Ki | Bioorg Med Chem (2008) 16: 8875-8881 [PMID:18793859] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1997) 40: 1-3 [PMID:9016321] |
ChEMBL | Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | B | 8.35 | pKi | 4.5 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
ChEMBL | Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | B | 8.35 | pKi | 4.5 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor by liquid scintillation counting | B | 8.38 | pKi | 4.2 | nM | Ki | Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
ChEMBL | Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
ChEMBL | Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells incubated for 60 mins by scintillation counting method | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.45 | pKi | 3.55 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin) | B | 8.45 | pKi | 3.55 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin) | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine receptor D2 long expressed in CHO cells | B | 8.48 | pKi | 3.3 | nM | Ki | Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913] |
ChEMBL | Displacement of [3H]Spiperone from human D2S receptor expressed in CHOK1 cell membranes measured after 120 mins | B | 8.49 | pKi | 3.25 | nM | Ki | Eur J Med Chem (2019) 180: 673-689 [PMID:31357129] |
ChEMBL | Displacement of [3H]spiperone form human dopamine D2 receptor by liquid scintillation counting | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2983-2986 [PMID:20347298] |
ChEMBL | Displacement of [3H]raclopride from human D2L receptor expressed in CHO cells after 60 mins by scintillation proximity assay | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]spiperone displacement. | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939] |
ChEMBL | Displacement of [3H]spiperone from D2 receptor | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5552-5555 [PMID:19720528] |
ChEMBL | Inhibition of human dopamine D2 receptor | B | 8.55 | pKi | 2.84 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2007) 50: 5043-5047 [PMID:17850060] |
ChEMBL | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity for human recombinant dopamine D2 receptor | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2004) 47: 4155-4158 [PMID:15293986] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 8.66 | pKi | 2.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
ChEMBL | In vitro inhibitory constant against [3H]spiperone binding to human dopamine D2 receptor expressed in CHO cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2005) 48: 6855-6869 [PMID:16250644] |
ChEMBL | Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Binding affinity to human D2 receptor | B | 8.71 | pKi | 1.97 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
ChEMBL | Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method | B | 8.73 | pKi | 1.86 | nM | Ki | J Med Chem (2021) 64: 12603-12629 [PMID:34436892] |
ChEMBL | Displacement of [3H]-methylspiperone from recombinant human D2 receptor expressed in CHOK1 cell membranes measured after 60 mins by microbeta counting method | B | 8.73 | pKi | 1.86 | nM | Ki | Eur J Med Chem (2020) 191: 112149-112149 [PMID:32105980] |
ChEMBL | Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1997) 40: 4026-4029 [PMID:9406594] |
GtoPdb | - | - | 8.8 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709] |
ChEMBL | Displacement of [3H]spiperone from human DRD2 Long receptor expressed in chinese hamster CHO cells by radioligand binding assay | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
ChEMBL | Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
ChEMBL | Displacement of [3H]SCH23390 from human D2long receptor expressed in CHO cells | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2011) 54: 4896-4903 [PMID:21599022] |
ChEMBL | Binding affinity for dopamine receptor D2 determined using [3H]spiperone | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728] |
ChEMBL | Displacement of [3H]-methylspiperone from human D2 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2017) 60: 7483-7501 [PMID:28763213] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Binding affinity towards human Dopamine receptor D2 | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2014) 57: 3450-3463 [PMID:24666157] |
ChEMBL | Binding affinity to human cloned dopamine D2 receptor | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Binding affinity for human dopamine receptor D2 long | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Binding affinity to dopamine D2 | B | 8.95 | pKi | 1.12 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2011) 54: 4896-4903 [PMID:21599022] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
ChEMBL | Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
ChEMBL | Displacement of [3H]spiperone from human DRD2 short receptor expressed in chinese hamster CHO cells by radioligand binding assay | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
ChEMBL | Binding affinity towards Dopamine type 2 receptor was determined by displacement assays using [3H]-YM 09151 as the competitive ligand | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
ChEMBL | Binding affinity towards mouse LtK- cells transfected with human D2 receptor using [3H]spiperone | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 219-222 |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells | B | 9.02 | pKi | 0.96 | nM | Ki | ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260] |
ChEMBL | Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test | B | 9.05 | pKi | 0.89 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 | B | 9.05 | pKi | 9.05 | nM | pKi | J Med Chem (2004) 47: 497-508 [PMID:14736232] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | B | 9.05 | pKi | 0.89 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice | B | 9.05 | pKi | 0.89 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells | B | 9.06 | pKi | 0.87 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
ChEMBL | Displacement of [3H]spiperone from human D2short receptor stably expressed in CHO cell membranes by competitive binding assay | B | 9.07 | pKi | 0.85 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579] |
ChEMBL | Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2014) 57: 4368-4381 [PMID:24779610] |
ChEMBL | In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 9.08 | pKi | 0.84 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
ChEMBL | Displacement of [3H]spiperone from human D2long receptor stably expressed in CHO cell membranes by competitive binding assay | B | 9.09 | pKi | 0.81 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579] |
ChEMBL | In vitro binding affinity for Dopamine receptor D2 | B | 9.1 | pKi | 0.79 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 9.15 | pKi | 0.7 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Inhibition of [3H]raclopride binding to Dopamine receptor D2 | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (1996) 39: 4421-4429 [PMID:8893836] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay | B | 9.22 | pKi | 0.6 | nM | Ki | Medchemcomm (2011) 2: 1194-1200 |
ChEMBL | Binding affinity towards dopamine receptor D2 | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]spiperone from human D2 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | Eur J Med Chem (2014) 71: 237-249 [PMID:24316025] |
ChEMBL | Displacement of [3H]spiperone human cloned dopamine D2 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
ChEMBL | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (2019) 62: 9488-9520 [PMID:31580666] |
ChEMBL | Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D2 | B | 9.36 | pKi | 0.44 | nM | Ki | J Med Chem (1993) 36: 3929-3936 [PMID:7902870] |
ChEMBL | Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells | B | 9.36 | pKi | 0.44 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538] |
ChEMBL | Displacement of [3H]spiperone from human D2long receptor expressed in CHO cell membranes by radioligand binding assay | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method | B | 9.58 | pKi | 0.26 | nM | Ki | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
ChEMBL | Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay | B | 9.6 | pKi | 0.25 | nM | Ki | Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858] |
ChEMBL | Displacement of [3H]quinpirole from Dopamine receptor D2 | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (1996) 39: 4421-4429 [PMID:8893836] |
ChEMBL | Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538] |
ChEMBL | Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
ChEMBL | Antagonist activity at dopamine D2 receptor (unknown origin) | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
ChEMBL | Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay | F | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346] |
ChEMBL | Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole | F | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 8.18 | pIC50 | 6.59 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity towards human Dopamine receptor D2 | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement. | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
ChEMBL | Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
ChEMBL | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | B | 9.15 | pIC50 | 0.71 | nM | IC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
ChEMBL | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
ChEMBL | Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay | B | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2014) 57: 7042-7060 [PMID:25126833] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Binding affinity towards dopamine receptor D2 was determined by displacement of [3H]spiroperidol from bovine nucleus caudate membranes. | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1987) 30: 814-819 [PMID:2883318] |
ChEMBL | Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170 | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1993) 36: 912-918 [PMID:8096548] |
ChEMBL | Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1992) 35: 2712-2715 [PMID:1353116] |
ChEMBL | Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding. | B | 8.01 | pKi | 9.8 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Binding affinity for dopamine receptor D2 long expressed in Sf9 cells using [125I]IABN radioligand | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (2001) 44: 1815-1826 [PMID:11356115] |
ChEMBL | Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 913-918 |
ChEMBL | Inhibition of [3H]-spiperone 23390 binding to dopamine receptor D2 rat striatal membrane | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1994) 37: 2564-2573 [PMID:7914540] |
ChEMBL | Inhibition constant for in vitro inhibition of [3H]spiperone binding to striatal membranes Dopamine receptor D2 | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 579-584 |
ChEMBL | Compound was evaluated for its affinity (pKi) to inhibit [3H]spiperone binding to the Dopamine receptor D2 | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1991) 34: 2242-2247 [PMID:1676759] |
GtoPdb | - | - | 8.3 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
ChEMBL | Compound was tested for its binding affinity towards Dopamine receptor D2 using [3H]spiperone from rat striatum | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1998) 41: 1557-1560 [PMID:9572880] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Inhibition of [3H]spiperone binding to rat dopamine D2 receptor | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | B | 8.32 | pKi | 4.79 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Displacement of [3H]YM-09151-2 from rat striatum D2 receptor | B | 8.36 | pKi | 4.37 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
ChEMBL | In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1987) 30: 1818-1823 [PMID:2888898] |
ChEMBL | In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1987) 30: 1100-1105 [PMID:2884314] |
ChEMBL | In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane. | B | 8.48 | pKi | 3.31 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2 | B | 8.48 | pKi | 3.31 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473] |
ChEMBL | Affinity against Dopamine receptor D2 | B | 8.48 | pKi | 3.31 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Binding affinity towards Dopamine receptor D2 in rat frontal striatum using [3H]spiperone | B | 8.53 | pKi | 2.95 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418] |
ChEMBL | Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone | B | 8.57 | pKi | 2.69 | nM | Ki | J Med Chem (2005) 48: 266-273 [PMID:15634021] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Displacement of [3H]-spiperone from DRD2 in rat striatum by scintillation counting | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2016) 59: 9960-9966 [PMID:27739690] |
ChEMBL | Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum by scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2015) 90: 1-9 [PMID:25461306] |
ChEMBL | Binding affinity to the dopamine receptor D2L in rat brain membranes | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1999) 42: 3342-3355 [PMID:10464021] |
ChEMBL | Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand. | B | 8.67 | pKi | 2.14 | nM | Ki | J Med Chem (2000) 43: 599-608 [PMID:10691686] |
ChEMBL | Displacement of [3H]-spiperone from dopamine D2 receptor in rat strriatum after 15 mins by liquid scintillation counting method | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2018) 61: 372-384 [PMID:29220177] |
ChEMBL | Displacement radioligand form dopamine D2 receptor in rat striatum by liquid scintillation counting | B | 8.68 | pKi | 2.1 | nM | Ki | Eur J Med Chem (2011) 46: 433-438 [PMID:21055848] |
ChEMBL | Inhibition of [3H]spiroperidol binding to Dopamine receptor D2 of rat striatal membranes | B | 8.71 | pKi | 1.95 | nM | Ki | J Med Chem (1998) 41: 1574-1580 [PMID:9572883] |
ChEMBL | Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
ChEMBL | Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand | B | 8.73 | pKi | 1.86 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
ChEMBL | In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 0.7 to 3.5 | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1987) 30: 1818-1823 [PMID:2888898] |
ChEMBL | Displacement of [3H]spiperone from Dopamine receptor D2 of rat corpora striata synaptic membranes | B | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1327-1330 |
ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 8.79 | pKi | 1.63 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1245-1250 |
ChEMBL | Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1988) 31: 1934-1940 [PMID:2902226] |
ChEMBL | Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1987) 30: 2099-2104 [PMID:2889830] |
ChEMBL | Affinity against the dopamine receptor D2 using [3H]spiperinone. | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1995) 38: 4211-4222 [PMID:7473548] |
ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Binding affinity was measured against dopamine (D2) receptor in rat using [3H]spiperone as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 9 | pKi | 1.01 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
ChEMBL | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
ChEMBL | Binding affinity against dopamine D2 receptor | B | 9.06 | pKi | 0.87 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | Binding affinity towards dopamine receptor D2 in rat striatal membranes | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2001) 44: 4431-4442 [PMID:11728188] |
ChEMBL | Binding affinity towards Dopamine receptor D2 | B | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (1997) 40: 586-593 [PMID:9046349] |
ChEMBL | Binding affinity was evaluated against Dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand; ND = Not determined | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1998) 41: 2765-2778 [PMID:9667967] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in rat brain | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521] |
ChEMBL | In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement. | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (1993) 36: 3073-3076 [PMID:7901415] |
ChEMBL | Binding affinity against dopamine receptor D2 from rat corpus striatum by using radioligand [3H]sulpiride | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (1993) 36: 1488-1495 [PMID:8496917] |
ChEMBL | Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
ChEMBL | Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (1998) 41: 1997-2009 [PMID:9622541] |
ChEMBL | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
ChEMBL | Affinity for Dopamine receptor D2 | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525] |
ChEMBL | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
ChEMBL | In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1994) 37: 2552-2563 [PMID:7914539] |
ChEMBL | Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata. | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1996) 39: 149-157 [PMID:8568802] |
ChEMBL | Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum | B | 7.49 | pIC50 | 32.7 | nM | IC50 | J Med Chem (1994) 37: 2308-2314 [PMID:7914536] |
ChEMBL | Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1991) 34: 1068-1072 [PMID:1672156] |
ChEMBL | Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum. | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1995) 38: 1119-1131 [PMID:7707315] |
ChEMBL | In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand | B | 7.76 | pIC50 | 17.5 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
ChEMBL | Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 | B | 7.86 | pIC50 | 13.7 | nM | IC50 | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1985) 28: 1263-1269 [PMID:4040977] |
ChEMBL | In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes. | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
ChEMBL | Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2 | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (1992) 35: 1092-1101 [PMID:1348090] |
ChEMBL | Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol. | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (1995) 38: 1998-2008 [PMID:7783131] |
ChEMBL | Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1986) 29: 359-369 [PMID:2869146] |
ChEMBL | In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1992) 35: 4516-4525 [PMID:1361578] |
ChEMBL | Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
ChEMBL | Compound was tested for its binding affinity towards Dopamine receptor D2 by using [3H]domperidone as radioligand | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (1991) 34: 3360-3365 [PMID:1662725] |
ChEMBL | Affinity towards Dopamine receptor D2 was evaluated in rat striatal membrane using [3H]spiperone as radioligand | B | 8.32 | pIC50 | 4.8 | nM | IC50 | J Med Chem (1996) 39: 4928-4934 [PMID:8960552] |
ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 8.32 | pIC50 | 4.8 | nM | IC50 | J Med Chem (1996) 39: 3195-3202 [PMID:8759642] |
ChEMBL | Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2 | B | 8.37 | pIC50 | 4.24 | nM | IC50 | J Med Chem (1991) 34: 194-197 [PMID:1671414] |
ChEMBL | Ability to inhibit the specific binding of [3H]- spiroperidol to Dopamine receptor D2 in rat striatal membrane preparation by 50% | B | 8.37 | pIC50 | 4.24 | nM | IC50 | J Med Chem (1987) 30: 1906-1910 [PMID:2888899] |
ChEMBL | Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand. | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1991) 34: 1860-1866 [PMID:1676427] |
ChEMBL | Displacement of [3H]spiroperidol from D2 dopamine receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (1994) 37: 1320-1325 [PMID:8176710] |
ChEMBL | Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
ChEMBL | In vivo binding affinity against dopamine (D2) receptor in rat caudate-putamen tissue using [3H]nemonapride as radioligand | B | 10.12 | pIC50 | 0.07 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497] |
Dopamine D3 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304406] [UniProtKB: P52703] | ||||||||
ChEMBL | Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3 | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1995) 38: 4950-4952 [PMID:8523409] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | F | 6.5 | pKd | 316.23 | nM | Kd | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
ChEMBL | Binding affinity of compound towards Dopamine receptor D3 using [3H]spiperone (1.2 nM) ligand in cortex was determined | B | 6.94 | pKi | 115 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK cells | B | 7.54 | pKi | 29 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
ChEMBL | Displacement of the radioligand [3H]YM-09151-2 from cloned human Dopamine receptor D3 expressed in CHO cells | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769] |
ChEMBL | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 7.64 | pKi | 22.91 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis | B | 7.79 | pKi | 16.04 | nM | Ki | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2007) 50: 5043-5047 [PMID:17850060] |
ChEMBL | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
ChEMBL | Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 7.9 | pKi | 12.7 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor | B | 7.94 | pKi | 11.48 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Inhibition of human dopamine D3 receptor | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Binding affinity for human dopamine receptor D3 | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane | B | 8.08 | pKi | 8.32 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Binding affinity towards Chinese hamster ovary cells transfected with human D3 receptor using [3H]spiperone | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 219-222 |
ChEMBL | Binding affinity for human recombinant dopamine receptor D3 | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2004) 47: 4155-4158 [PMID:15293986] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 8.16 | pKi | 6.84 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 8.17 | pKi | 6.8 | nM | Ki | ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260] |
ChEMBL | Displacement of [3H]YM-09151-2 from human cloned dopamine D3 receptor expressed in CHO cells | B | 8.19 | pKi | 6.4 | nM | Ki | Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913] |
ChEMBL | Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2011) 54: 4896-4903 [PMID:21599022] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in chinese hamster CHO cells by radioligand binding assay | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | B | 8.24 | pKi | 5.75 | nM | Ki | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | B | 8.26 | pKi | 5.5 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | B | 8.29 | pKi | 5.16 | nM | Ki | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230] |
ChEMBL | In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test | B | 8.34 | pKi | 4.57 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Displacement of [3H]7-OH-DPAT from human Dopamine receptor D3 | B | 8.34 | pKi | 8.34 | nM | pKi | J Med Chem (2004) 47: 497-508 [PMID:14736232] |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
ChEMBL | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Displacement of [3H]raclopride from Dopamine receptor D3 | B | 8.56 | pKi | 2.74 | nM | Ki | J Med Chem (1996) 39: 4421-4429 [PMID:8893836] |
ChEMBL | Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3 | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
ChEMBL | Displacement of [3H]spiperone from human D3 receptor stably expressed in CHO cell membranes by competitive binding assay | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579] |
GtoPdb | - | - | 8.6 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting | B | 8.6 | pKi | 2.5 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | Binding affinity to human cloned dopamine D3 receptor | B | 8.6 | pKi | 2.5 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes by radioligand binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858] |
ChEMBL | Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1997) 40: 4026-4029 [PMID:9406594] |
ChEMBL | Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro. | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells. | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2014) 57: 3450-3463 [PMID:24666157] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method | B | 8.95 | pKi | 1.12 | nM | Ki | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
ChEMBL | Displacement of [3H]-spiperone from CHO-K1 cell membranes expressing human dopamine 3 receptors | B | 9.02 | pKi | 0.96 | nM | Ki | J Med Chem (1993) 36: 3929-3936 [PMID:7902870] |
ChEMBL | Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Tested for binding affinity towards human D3 receptor using [3H]spiperone as radioligand | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.7 | pIC50 | 20 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay | F | 8.46 | pIC50 | 3.47 | nM | IC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
ChEMBL | Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay | B | 10.22 | pIC50 | 0.06 | nM | IC50 | J Med Chem (2014) 57: 7042-7060 [PMID:25126833] |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
ChEMBL | Binding affinity for dopamine receptor D3 expressed in Sf9 cells using [125I]IABN the radioligand. | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2001) 44: 1815-1826 [PMID:11356115] |
ChEMBL | Binding affinity towards Dopamine receptor D3 of rat using [3H]spiroperidol as radioligand | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
ChEMBL | Displacement of [3H]PD 128907 from rat ventral striatal membrane dopamine D3-like receptor | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 443-446 [PMID:16290142] |
ChEMBL | Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | B | 7.74 | pKi | 18.2 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 7.84 | pKi | 14.3 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
ChEMBL | Displacement of [3H]-7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle by scintillation counting method | B | 8.06 | pKi | 8.8 | nM | Ki | Eur J Med Chem (2015) 90: 1-9 [PMID:25461306] |
ChEMBL | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]-7-OH-DPAT from DRD3 in rat olfactory tubercle by scintillation counting | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2016) 59: 9960-9966 [PMID:27739690] |
ChEMBL | Displacement radioligand form dopamine D3 receptor in rat olfactory tubercle by liquid scintillation counting | B | 8.24 | pKi | 5.8 | nM | Ki | Eur J Med Chem (2011) 46: 433-438 [PMID:21055848] |
ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 8.25 | pKi | 5.57 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 8.3 | pKi | 5.04 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity towards baculovirus expressed rat dopamine D3 receptors | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) | B | 6.7 | pKi | 198 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells | B | 6.99 | pKi | 103 | nM | Ki | Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913] |
ChEMBL | Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells | B | 7.38 | pKi | 42 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769] |
ChEMBL | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 7.58 | pKi | 26.3 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 7.58 | pKi | 26.3 | nM | Ki | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
ChEMBL | Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting | B | 7.9 | pKi | 12.7 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
ChEMBL | Binding affinity towards human dopamine-4.2 receptor | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 | B | 7.98 | pKi | 7.98 | nM | pKi | J Med Chem (2004) 47: 497-508 [PMID:14736232] |
ChEMBL | Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test | B | 7.98 | pKi | 10.47 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Inhibition of human dopamine D4 receptor | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Binding affinity for human recombinant dopamine receptor D4.2 | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (2004) 47: 4155-4158 [PMID:15293986] |
ChEMBL | Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (1997) 40: 1-3 [PMID:9016321] |
ChEMBL | Binding affinity for Dopamine receptor D4 | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Displacement of [3H]-YM 09151 from human Dopamine receptor D4 | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (1995) 38: 4950-4952 [PMID:8523409] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
ChEMBL | Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2011) 54: 4896-4903 [PMID:21599022] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane | B | 8.22 | pKi | 6.03 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
ChEMBL | Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579] |
ChEMBL | Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
ChEMBL | Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding. | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
ChEMBL | Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1327-1330 |
ChEMBL | Binding affinity to human cloned dopamine D4 receptor | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Inhibition of human dopamine D4 receptor | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1997) 40: 4026-4029 [PMID:9406594] |
ChEMBL | Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
ChEMBL | In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4 | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206] |
ChEMBL | In vitro binding affinity for Dopamine receptor D4 | B | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544] |
GtoPdb | - | - | 8.8 | pKi | - | - | - |
Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.84 | pKi | 1.43 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
ChEMBL | In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206] |
ChEMBL | In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement. | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
ChEMBL | Binding affinity towards human Dopamine receptor D4.2 in CHO cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand | B | 9.13 | pKi | 0.74 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
ChEMBL | DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) | B | 6.25 | pIC50 | 563 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity towards human D4.2 receptor | B | 8.19 | pIC50 | 6.5 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement. | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
ChEMBL | Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5 | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206] |
ChEMBL | Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay | F | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2921-2924 [PMID:14611858] |
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
GtoPdb | - | - | 6.3 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Binding affinity for human recombinant dopamine receptor D5 | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2004) 47: 4155-4158 [PMID:15293986] |
ChEMBL | Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells | B | 7.32 | pKi | 48 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
ChEMBL | Inhibition of human dopamine D5 receptor | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM | B | 6.29 | pKi | 512 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150] |
ChEMBL | Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Inhibitory concentration against IKr potassium channel | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
ChEMBL | Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay | B | 5.94 | pIC50 | 1160 | nM | IC50 | J Med Chem (2020) 63: 5734-5751 [PMID:32392053] |
ChEMBL | Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319] |
ChEMBL | Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Nat Prod (2012) 75: 1210-1214 [PMID:22694270] |
ChEMBL | Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 7.52 | pIC50 | 30.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 7.52 | pIC50 | 30.2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 7.52 | pIC50 | 30.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state | F | 7.55 | pIC50 | 28.18 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 7.55 | pIC50 | 28.18 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 7.55 | pIC50 | 28.1 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
ChEMBL | Inhibition of hERG K channel | F | 7.57 | pIC50 | 27 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
ChEMBL | Inhibition of human ERG | B | 7.57 | pIC50 | 26.92 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
ChEMBL | Inhibition of human ERG channel | B | 7.57 | pIC50 | 26.8 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
ChEMBL | Inhibition of human ERG channel | B | 7.57 | pIC50 | 26.8 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
ChEMBL | Inhibition of human ERG | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
GtoPdb | - | - | 6.1 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
ChEMBL | Binding affinity towards human histamine H1 receptor | B | 6.14 | pKi | 730 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity to human cloned histamine H1 receptor | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230] |
ChEMBL | Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 6.49 | pKi | 323 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 5.56 | pIC50 | 2781 | nM | IC50 | DrugMatrix in vitro pharmacology data |
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
ChEMBL | Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay. | B | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate | B | 6.42 | pKi | 384 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine | B | 6.42 | pKi | 384 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Displacement of [3H]mepyramine from H1R in rat brain | B | 5.7 | pIC50 | >2000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666] |
ChEMBL | Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.94 | pKi | 1147 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.93 | pIC50 | 1166 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Histone H1.0 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707465] [UniProtKB: P07305] | ||||||||
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 6.11 | pKi | 780 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
HLA class I histocompatibility antigen A-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2632] [UniProtKB: P04439] | ||||||||
ChEMBL | Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay | B | 5 | pKd | <10000 | nM | Kd | Bioorg Med Chem Lett (2018) 28: 2837-2841 [PMID:30077568] |
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874] | ||||||||
ChEMBL | Binding affinity to HIV-1 protease | B | 4 | pKi | 100000 | nM | Ki | J Med Chem (1994) 37: 1769-1778 [PMID:8021917] |
ChEMBL | Binding affinity for HIV-1 protease | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1991) 34: 2305-2314 [PMID:1875332] |
Human rhinovirus A protease in Human rhinovirus sp. (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2857] [UniProtKB: Q4U254] | ||||||||
ChEMBL | The compound was tested for its affinity against HIV-2 protease | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1991) 34: 2305-2314 [PMID:1875332] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay | B | 5.61 | pKi | 2470 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 6 | pKi | 992 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.61 | pIC50 | 2443 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Binding affinity to human cloned muscarinic M1 receptor | B | 5.8 | pKi | 1600 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting | B | 5.8 | pKi | 1600 | nM | Ki | Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230] |
ChEMBL | Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
ChEMBL | Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Binding affinity was measured against muscarinic (M1) receptor in rat using [3H]pirenzepine as radioligand | B | 5.67 | pKi | 2140 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
ChEMBL | Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay. | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
ChEMBL | Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand | B | 5.21 | pKi | 6120 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
ChEMBL | Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by quinuclidinyl binding assay. | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes | B | 6.62 | pKi | 238 | nM | Ki | J Med Chem (1998) 41: 1574-1580 [PMID:9572883] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.55 | pKi | 2795 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.41 | pIC50 | 3890 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting | B | 5.26 | pKi | 5500 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.74 | pKi | 1820 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.74 | pIC50 | 1836 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
ChEMBL | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | B | 5.28 | pIC50 | 5300 | nM | IC50 | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069] | ||||||||
ChEMBL | Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (2016) 59: 5149-5157 [PMID:26588045] |
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156] | ||||||||
ChEMBL | Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 3563-3564 [PMID:12904059] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to human cloned 5HT1A receptor | B | 5.44 | pKi | 3600 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H] 8-OH-DPAT from human 5-HT1A receptor by liquid scintillation counting | B | 5.44 | pKi | 3600 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand | B | 5.55 | pKi | 2800 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 5.77 | pKi | 1703 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
GtoPdb | - | - | 5.8 | pKi | - | - | - |
Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; J Pharmacol Exp Ther (1997) 280: 1241-9 [PMID:9067310]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398] |
ChEMBL | Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding. | B | 5.08 | pKi | 8400 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand | B | 5.24 | pKi | 5750 | nM | Ki | J Med Chem (1992) 35: 2712-2715 [PMID:1353116] |
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes. | B | 5.62 | pKi | 2390 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
ChEMBL | Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay. | B | 5.72 | pKi | 1900 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor | B | 5.74 | pKi | 1800 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1245-1250 |
ChEMBL | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | B | 5.77 | pKi | 1698.24 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
ChEMBL | Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1997-2009 [PMID:9622541] |
ChEMBL | The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M. | B | 6.3 | pKi | >500 | nM | Ki | J Med Chem (1999) 42: 3342-3355 [PMID:10464021] |
ChEMBL | Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101 | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
ChEMBL | Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101. | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (1995) 38: 4211-4222 [PMID:7473548] |
ChEMBL | The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand | B | 5.15 | pIC50 | 7079 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus | B | 5.15 | pIC50 | 7079 | nM | IC50 | J Med Chem (1994) 37: 2308-2314 [PMID:7914536] |
ChEMBL | In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (1994) 37: 2552-2563 [PMID:7914539] |
ChEMBL | Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue. | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (1996) 39: 149-157 [PMID:8568802] |
ChEMBL | Compound was measured for affinity at 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue | B | 5.21 | pIC50 | 6210 | nM | IC50 | J Med Chem (1991) 34: 1068-1072 [PMID:1672156] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (1995) 38: 1998-2008 [PMID:7783131] |
ChEMBL | In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand | B | 5.7 | pIC50 | 1993 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand. | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1991) 34: 1860-1866 [PMID:1676427] |
ChEMBL | Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | B | 6.36 | pKi | 435 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | B | 6.78 | pKi | 165.96 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay | B | 6.78 | pKi | 165.96 | nM | Ki | Medchemcomm (2011) 2: 1194-1200 |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | B | 6.78 | pKi | 165.96 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor | B | 6.78 | pKi | 165.96 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor | B | 6.78 | pKi | 165.96 | nM | Ki | Eur J Med Chem (2014) 71: 237-249 [PMID:24316025] |
ChEMBL | Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor | B | 6.78 | pKi | 165.96 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation counting | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | Binding affinity to human cloned 5HT2A receptor | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Binding affinity towards human 5-HT2A receptor in BEK cells | B | 6.97 | pKi | 108 | nM | Ki | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 7 | pKi | 100 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method | B | 7.05 | pKi | 89 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
GtoPdb | - | - | 7.3 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method | B | 7.64 | pKi | 22.91 | nM | Ki | J Med Chem (2021) 64: 12603-12629 [PMID:34436892] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 7.68 | pKi | 21 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibitory concentration against human 5-HT2A receptor in BEK cells | B | 6.54 | pIC50 | 288 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 7.12 | pIC50 | 75 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129] | ||||||||
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2010) 53: 7219-7228 [PMID:20839776] |
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
ChEMBL | Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | B | 6.78 | pKi | 165.96 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand | B | 6.79 | pKi | 164 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay. | B | 7.06 | pKi | 87 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]ketanserin from rat cortex 5HT2A receptor | B | 7.08 | pKi | 83.18 | nM | Ki | J Med Chem (2007) 50: 865-876 [PMID:17300168] |
ChEMBL | Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding. | B | 7.12 | pKi | 75 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin | B | 7.28 | pKi | 52.48 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418] |
ChEMBL | In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor | B | 7.28 | pKi | 52.48 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex | B | 7.28 | pKi | 52.48 | nM | Ki | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
ChEMBL | In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain. | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor | B | 7.35 | pKi | 44.67 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
GtoPdb | - | - | 7.4 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat brain | B | 7.46 | pKi | 34.67 | nM | Ki | Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521] |
ChEMBL | In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane. | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor) | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473] |
ChEMBL | Inhibition constant for in vitro inhibition of [3H]ketanserin binding to rat frontal cortex membranes 5-hydroxytryptamine 2A receptor | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 579-584 |
ChEMBL | Serotonergic activity of the compound. | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (2000) 43: 3233-3243 [PMID:10966742] |
ChEMBL | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (1994) 37: 2564-2573 [PMID:7914540] |
ChEMBL | Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 913-918 |
ChEMBL | In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex | B | 6.89 | pIC50 | 129 | nM | IC50 | J Med Chem (1994) 37: 2308-2314 [PMID:7914536] |
ChEMBL | In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
ChEMBL | Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (1995) 38: 1998-2008 [PMID:7783131] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.88 | pKi | 1305 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 6.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.69 | pIC50 | 2050 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Displacement of [3H]mesulergine from human cloned 5HT2C receptor | B | 5.14 | pKi | 7244.36 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor | B | 5.14 | pKi | 7244.36 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor | B | 5.14 | pKi | 7244.36 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor | B | 5.14 | pKi | 7244.36 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity to human cloned 5HT2C receptor | B | 5.33 | pKi | 4700 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus | B | 5.34 | pKi | 4570.88 | nM | Ki | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
ChEMBL | In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor | B | 5.34 | pKi | 4570.88 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 5.4 | pKi | 3949 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus. | B | 5.6 | pKi | 2511.89 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.76 | pKi | 1753 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.48 | pIC50 | 3347 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
ChEMBL | Displacement of [3H]Mesulergine from rat 5-HT2C receptor by liquid scintillation counting | B | 5.33 | pKi | 4700 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979] | ||||||||
ChEMBL | Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Binding affinity to human cloned 5HT6 receptor | B | 5.22 | pKi | 6000 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 5.97 | pKi | 1083 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method | B | 5.95 | pKi | 1122.02 | nM | Ki | Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609] |
ChEMBL | Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method | B | 5.96 | pKi | 1100 | nM | Ki | Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609] |
ChEMBL | Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 6.39 | pKi | 408 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
GtoPdb | - | - | 6.6 | pKi | - | - | - | Br J Pharmacol (1997) 122: 126-32 [PMID:9298538] |
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
GtoPdb | - | - | 6.3 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 6.58 | pKi | 263 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
GtoPdb | - | - | 6.6 | pKi | - | - | - |
Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Binding affinity to human SERT | B | 5.74 | pKi | 1800 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]Citalopram from human Serotonin transporter by liquid scintillation counting | B | 5.74 | pKi | 1800 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422] |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.74 | pKi | 1799 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 6 | pKi | >1000 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.47 | pIC50 | 3386 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
ChEMBL | In vitro binding affinity for serotonin reuptake sites in rat frontal cortex membranes by [3H]paroxetine displacement. | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H](+)pentazocine from sigma-1 receptor in Cavia porcellus (guinea pig) brain membranes | B | 8.04 | pKi | 9.2 | nM | Ki | Med Chem Res (2005) 14: 158-168 |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
ChEMBL | Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | B | 8.18 | pKi | 6.6 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting method | B | 8.18 | pKi | 6.6 | nM | Ki | Eur J Med Chem (2016) 121: 712-726 [PMID:27366902] |
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2016) 59: 5505-5519 [PMID:27156565] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from guinea pig Sigma1-receptor after 120 mins by liquid scintillation counting method | B | 8.18 | pKi | 6.6 | nM | Ki | Medchemcomm (2016) 7: 317-326 |
ChEMBL | Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer | B | 8.18 | pKi | 6.6 | nM | Ki | Eur J Med Chem (2015) 90: 797-808 [PMID:25528334] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2014) 57: 2884-2894 [PMID:24617836] |
ChEMBL | Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor guinea pig brain after 180 mins scintillation counting | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2010) 18: 8005-8015 [PMID:20965739] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by scintillation counting | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2011) 19: 393-405 [PMID:21126878] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain by scintillation analyzer | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2011) 19: 3141-3151 [PMID:21531141] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 180 mins by solid scintillation counting | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2012) 20: 257-269 [PMID:22136765] |
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2013) 21: 1844-1856 [PMID:23462714] |
ChEMBL | Displacement of (+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2013) 69: 490-497 [PMID:24095744] |
ChEMBL | Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2014) 83: 526-533 [PMID:24996139] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2014) 22: 6638-6646 [PMID:25458498] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain cortex membranes | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2014) 22: 4277-4284 [PMID:24913984] |
ChEMBL | Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guniea pig brain cortex membranes by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5748-5751 [PMID:26531150] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation spectrometry | B | 8.2 | pKi | 6.3 | nM | Ki | Medchemcomm (2016) 7: 327-331 |
ChEMBL | Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain homogenate incubated for 120 mins by solid scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2016) 116: 136-146 [PMID:27061977] |
ChEMBL | Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by liquid scintillation counting | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962] |
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2017) 25: 5365-5372 [PMID:28797770] |
ChEMBL | Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes incubated for 120 mins measured for 5 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2018) 144: 672-681 [PMID:29289890] |
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 8.2 | pKi | 6.3 | nM | Ki | Medchemcomm (2017) 8: 975-981 [PMID:30108812] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2019) 180: 268-282 [PMID:31319263] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876] |
ChEMBL | Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2019) 177: 47-62 [PMID:31129453] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917] |
ChEMBL | Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by liquid scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method | B | 8.2 | pKi | 6.3 | nM | Ki | Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain homogenates | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2012) 55: 8953-8957 [PMID:23013229] |
ChEMBL | Displacement of [3H]pentazocine from guinea pig sigma1 receptor measured after 90 mins by microbeta scintillation counting method | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5689-5694 [PMID:27839919] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane incubated for 120 mins measured for 5 mins by scintillation counting method | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma-1 receptor after 180 mins by scintillation counting analysis | B | 8.41 | pKi | 3.9 | nM | Ki | Medchemcomm (2012) 3: 673-679 |
ChEMBL | Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in guinea pig brain homogenate | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2009) 17: 777-793 [PMID:19081725] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain after 180 mins by scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | Eur J Med Chem (2009) 44: 4306-4314 [PMID:19709783] |
ChEMBL | Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2011) 54: 6704-6713 [PMID:21859078] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by scintillation analysis | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2009) 52: 2126-2137 [PMID:19243173] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2012) 55: 8047-8065 [PMID:22913577] |
ChEMBL | Displacement of [3H]-(+)pentazocine from guinea pig brain sigma 1-type opioid receptor after 120 mins by scintillation counting analysis | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2012) 55: 5350-5360 [PMID:22515405] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 180 mins by solid scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | Eur J Med Chem (2012) 53: 327-336 [PMID:22578786] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by solid scintillation analysis | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2009) 17: 3630-3641 [PMID:19394833] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 180 mins by scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2009) 52: 6062-6072 [PMID:19791807] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2008) 51: 6531-6537 [PMID:18816044] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 opioid receptor in guinea pig brain by solid scintillation counting | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2009) 17: 1445-1455 [PMID:19196515] |
ChEMBL | Displacement of [3H](+)-pentazocine from Sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 2676-2679 [PMID:27090556] |
ChEMBL | Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 1 mM DPH by liquid scintillation counting method | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2017) 125: 603-610 [PMID:27721146] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method | B | 8.49 | pKi | 3.27 | nM | Ki | Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607] |
ChEMBL | Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis | B | 8.55 | pKi | 2.8 | nM | Ki | Eur J Med Chem (2013) 64: 488-497 [PMID:23680866] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 150 mins by liquid scintillation counting method | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem (2016) 24: 3149-3156 [PMID:27262426] |
ChEMBL | Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 250 uM DPH by liquid scintillation counting method | B | 8.57 | pKi | 2.7 | nM | Ki | Eur J Med Chem (2017) 125: 603-610 [PMID:27721146] |
ChEMBL | Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2016) 59: 9960-9966 [PMID:27739690] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Dunkin Hartley guinea pig membrane after 180 mins by liquid scintillation counting analysis | B | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2014) 79: 216-230 [PMID:24735647] |
ChEMBL | Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of DPH solvent by liquid scintillation counting method | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2017) 125: 603-610 [PMID:27721146] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method | B | 8.6 | pKi | 2.5 | nM | Ki | Eur J Med Chem (2015) 90: 1-9 [PMID:25461306] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation counting method | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2017) 60: 9531-9544 [PMID:29172528] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | B | 8.6 | pKi | 2.5 | nM | Ki | ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2011) 46: 433-438 [PMID:21055848] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2011) 54: 3669-3673 [PMID:21476493] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2018) 61: 372-384 [PMID:29220177] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2009) 44: 519-525 [PMID:18499305] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by microbeta scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2021) 64: 13622-13632 [PMID:34477381] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in guinea pig brain membrane | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem (2008) 16: 2992-3001 [PMID:18221879] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 2 hrs by scintillation counting | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem (2016) 24: 4045-4055 [PMID:27396684] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2007) 50: 6144-6153 [PMID:17967001] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 150 mins by scintillation counting method | B | 8.8 | pKi | 1.6 | nM | Ki | Eur J Med Chem (2019) 174: 226-235 [PMID:31042618] |
ChEMBL | Displacement of [3H]-pentazocine from guinea pig sigma1 receptor by liquid scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2011) 54: 1555-1564 [PMID:21348515] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting | B | 8.84 | pKi | 1.45 | nM | Ki | Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1-type opioid receptor in guinea pig brain homogenates | B | 8.84 | pKi | 1.45 | nM | Ki | Bioorg Med Chem (2009) 17: 1222-1231 [PMID:19119012] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem (2014) 22: 393-397 [PMID:24290063] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from Sigma1-receptor in guinea pig brain membrane | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem (2011) 19: 1852-1859 [PMID:21376604] |
ChEMBL | Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem (2008) 16: 755-761 [PMID:18029187] |
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
ChEMBL | Binding affinity to sigma-2 receptor (unknown origin) | B | 6.66 | pKi | 221 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
ChEMBL | Displacement of [3H]-DTG from sigma-2 receptor in human Jurkat cell membrane incubated for 1 hr by liquid scintillation counting method | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
ChEMBL | Displacement of [3H]-DTG from sigma2 receptor (unknown origin) incubated for 120 mins by scintillation counting method | B | 7.75 | pKi | 17.6 | nM | Ki | Eur J Med Chem (2019) 174: 226-235 [PMID:31042618] |
ChEMBL | Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) after 120 mins by liquid scintillation counting method | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2017) 60: 9531-9544 [PMID:29172528] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method | B | 7.8 | pKi | 16 | nM | Ki | ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401] |
σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7] | ||||||||
ChEMBL | Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay | B | 7.09 | pKi | 80.6 | nM | Ki | Eur J Med Chem (2019) 165: 250-257 [PMID:30685525] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins measured for 5 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613] |
ChEMBL | Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by liquid scintillation counting | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962] |
ChEMBL | Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894] |
ChEMBL | Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membranes after 120 mins by scintillation counting analysis | B | 7.11 | pKi | 78 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2018) 144: 672-681 [PMID:29289890] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes in the presence of sigma1 receptor ligand (+)-pentazocine incubated for 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2019) 180: 268-282 [PMID:31319263] |
ChEMBL | Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876] |
ChEMBL | Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496] |
ChEMBL | Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2019) 177: 47-62 [PMID:31129453] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane by solid scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806] |
ChEMBL | Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins by liquid scintillation counting method relative to control | B | 7.11 | pKi | 78 | nM | Ki | Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494] |
ChEMBL | Displacement of [3H]DTG from sigma-2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431] |
ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins in the presence of sigma1 receptor ligand (+)-pentazocine by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460] |
ChEMBL | Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method | B | 7.11 | pKi | 78 | nM | Ki | ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366] |
ChEMBL | Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method | B | 7.36 | pKi | 43.9 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
ChEMBL | Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method | B | 7.45 | pKi | 35.22 | nM | Ki | Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607] |
ChEMBL | Displacement of (+)-[3H]DTG from sigma 2 receptor in SPRD rat liver membrane incubated for 2 hrs by liquid scintillation counting method | B | 7.69 | pKi | 20.5 | nM | Ki | RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2014) 57: 2884-2894 [PMID:24617836] |
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in human RPMI8226 cell membranes | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2016) 59: 5505-5519 [PMID:27156565] |
ChEMBL | Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2005) 48: 266-273 [PMID:15634021] |
ChEMBL | Displacement of [3H](+)-pentazocine from human sigma 1 receptor in human Jurkat cell membranes incubated for 2 hrs by liquid scintillation counting | B | 7.92 | pKi | 11.9 | nM | Ki | Eur J Med Chem (2015) 89: 198-206 [PMID:25462240] |
ChEMBL | Displacement of [3H](+)Pentazocine from sigma 1 receptor in human Jurkat cells after 120 mins by liquid scintillation counting analysis | B | 7.92 | pKi | 11.9 | nM | Ki | Eur J Med Chem (2015) 92: 575-582 [PMID:25602932] |
ChEMBL | The compound was tested for its binding affinity towards Sigma opioid receptor in guinea pig brain membranes | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1991) 34: 3360-3365 [PMID:1662725] |
ChEMBL | Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs | B | 8.06 | pKi | 8.8 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in human Jurkat cell membrane | B | 8.11 | pKi | 7.76 | nM | Ki | J Med Chem (2010) 53: 1261-1269 [PMID:20067271] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed in HEK293 cell membranes after 120 mins by microbeta scintillation counting method | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem (2019) 27: 1824-1835 [PMID:30904383] |
ChEMBL | Binding affinity to sigma-1 receptor (unknown origin) | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
ChEMBL | Binding affinity to sigma-1 receptor (unknown origin) by radioligand displacement assay | B | 8.2 | pKi | 6.3 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 889-893 [PMID:26750254] |
ChEMBL | Binding affinity for Sigma opioid receptor type 2 in guinea pig brain homogenate with 4 nM [3H]-(+)-DTG | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2185-2188 |
ChEMBL | Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 8.25 | pKi | 5.67 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of [3H]DTG binding to Sigma opioid receptor | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1991) 34: 1855-1859 [PMID:1648139] |
ChEMBL | Binding affinity against sigma receptor of MCF cells | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (1994) 37: 1737-1739 [PMID:8021913] |
ChEMBL | Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (1996) 39: 176-182 [PMID:8568804] |
ChEMBL | Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1993) 36: 2311-2320 [PMID:8360875] |
ChEMBL | Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1993) 36: 566-571 [PMID:8496936] |
ChEMBL | Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1994) 37: 314-321 [PMID:8295220] |
ChEMBL | Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1992) 35: 4334-4343 [PMID:1447735] |
ChEMBL | Compound was evaluated for its in vitro competition binding studies using sigma-ligand (0.05-10000 nM) - [3H](+)-pentazocine (sigma1 receptor) in guinea pig brain membranes | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1998) 41: 2445-2450 [PMID:9651150] |
ChEMBL | Displacement of [3H]pentazocine from human sigma 1 receptor expressed in HEK293 cell membrane incubated for 2 hrs by liquid scintillation counting method | B | 8.45 | pKi | 3.53 | nM | Ki | RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165] |
ChEMBL | Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (1998) 41: 1557-1560 [PMID:9572880] |
ChEMBL | Compound tested for binding affinity towards sigma 1 receptor in quinea pig brain membranes using [3H](+)-pentazocine as the radioligand. | B | 8.6 | pKi | 2.53 | nM | Ki | J Med Chem (1998) 41: 2361-2370 [PMID:9632369] |
ChEMBL | Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand | B | 8.6 | pKi | 2.53 | nM | Ki | J Med Chem (2001) 44: 4404-4415 [PMID:11728186] |
ChEMBL | Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes | B | 8.61 | pKi | 2.46 | nM | Ki | Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780] |
ChEMBL | Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes | B | 8.61 | pKi | 2.46 | nM | Ki | Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780] |
ChEMBL | Displacement of [3H]-pentazocine from sigma-1 receptor in human Jurkat cell membrane incubated for 2 hr by liquid scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
ChEMBL | Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2002) 45: 4923-4930 [PMID:12383018] |
ChEMBL | Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand. | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2002) 45: 438-448 [PMID:11784148] |
ChEMBL | Inhibitory constant against sigma receptor type 1 using 3 nM [3H]pentazocine | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2005) 48: 266-273 [PMID:15634021] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cells after 120 mins by liquid scintillation counting analysis | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2013) 56: 3656-3665 [PMID:23560650] |
ChEMBL | Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2012) 55: 8211-8224 [PMID:22784008] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2020) 63: 2434-2454 [PMID:31743642] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2020) 63: 14979-14988 [PMID:33237785] |
ChEMBL | Inhibition of sigma 1 receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Inhibition of [3H]- pentazocine binding against alpha-1 from guinea pig brain | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1999) 42: 5181-5187 [PMID:10602703] |
ChEMBL | Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin) | B | 8.78 | pKi | 1.66 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method | B | 8.8 | pKi | 1.6 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
ChEMBL | Inhibition of [3H]pentazocine binding to sigma-1 sites in guinea pig brain membranes | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1998) 41: 1574-1580 [PMID:9572883] |
ChEMBL | Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding. | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Binding affinity for sigma-1 receptor measured on guinea pig brain membranes using [3H](+)-pentazocine as radioligand | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2001) 44: 1815-1826 [PMID:11356115] |
ChEMBL | Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin) | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H](+)-pentazocine from human sigma1 receptor by PDSP assay | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890] |
ChEMBL | Binding affinity for Sigma opioid receptor type 1 in guinea pig brain homogenate with 0.5 nM [3H](+)-PENT | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2185-2188 |
ChEMBL | The compound was evaluated for affinity at sigma-1 site by inhibition of [3H](+)-pentazocine (PENT) binding in guinea pig brain. | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
ChEMBL | Inhibition of [3H]pentazocine binding to Sigma opioid receptor type 1 | B | 9.36 | pKi | 0.44 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2303-2306 |
ChEMBL | Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1993) 36: 3929-3936 [PMID:7902870] |
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes | B | 9.68 | pKi | 0.21 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2216-2220 [PMID:28385503] |
ChEMBL | Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting | B | 6.64 | pIC50 | 230 | nM | IC50 | Eur J Med Chem (2010) 45: 256-263 [PMID:19875205] |
ChEMBL | The compound was tested for affinity towards sigma-3 receptor | B | 6.67 | pIC50 | 213.8 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
ChEMBL | Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 7.89 | pIC50 | 13 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
ChEMBL | In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand | B | 8.25 | pIC50 | 5.64 | nM | IC50 | J Med Chem (1995) 38: 942-949 [PMID:7699710] |
ChEMBL | Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1991) 34: 1867-1870 [PMID:1648140] |
ChEMBL | Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
ChEMBL | Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
ChEMBL | Inhibitory activity against opioid receptor sigma 1 in guinea pig cerebral cortex using [3H](+)-pentazocine as radio ligand at pH 7.5 for 150 min at 22 degree C | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4828-4832 [PMID:16140009] |
ChEMBL | Inhibitory concentration against opioid receptor sigma 1 of guinea pig cerebral cortex using [3H](+)-pentazocine upon incubation for 150 minutes at 22 degree C | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4833-4837 [PMID:16140011] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
ChEMBL | Binding affinity was measured on Sigma receptor type 2 with rat liver membranes and [3H]- DTG as ligand. | B | 7.33 | pKi | 46.5 | nM | Ki | J Med Chem (2000) 43: 3913-3922 [PMID:11052796] |
ChEMBL | Binding affinity of compound towards sigma receptor using [3H]DTG (4 nM) ligand in hippocampus rat was determined | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver | B | 7.47 | pKi | 34.2 | nM | Ki | J Med Chem (2002) 45: 4923-4930 [PMID:12383018] |
ChEMBL | Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand | B | 7.47 | pKi | 34.2 | nM | Ki | J Med Chem (2002) 45: 438-448 [PMID:11784148] |
ChEMBL | Inhibitory activity against Opioid receptor sigma 1 isolated from whole rat membranes using [3H](+)-pentazocine as radioligand | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 176-182 [PMID:8568804] |
ChEMBL | Displacement of [3H]pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by microbeta scintillation counting analysis | B | 8.15 | pKi | 7 | nM | Ki | ACS Med Chem Lett (2012) 3: 1054-1058 [PMID:23641311] |
ChEMBL | Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting | B | 8.24 | pKi | 5.7 | nM | Ki | ACS Med Chem Lett (2011) 2: 834-839 [PMID:24900272] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane | B | 8.24 | pKi | 5.7 | nM | Ki | Eur J Med Chem (2009) 44: 124-130 [PMID:18440098] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (2009) 52: 5380-5393 [PMID:19673530] |
ChEMBL | Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method | B | 8.27 | pKi | 5.39 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
ChEMBL | Displacement of (+)-[3H]pentazocine from rat brain sigma1 receptor by competitive binding assay | B | 8.31 | pKi | 4.95 | nM | Ki | J Med Chem (2013) 56: 3478-3491 [PMID:23566245] |
ChEMBL | Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes | B | 8.31 | pKi | 4.95 | nM | Ki | Bioorg Med Chem (2013) 21: 215-222 [PMID:23199475] |
ChEMBL | Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins by radioligand binding assay | B | 8.47 | pKi | 3.35 | nM | Ki | Eur J Med Chem (2019) 165: 250-257 [PMID:30685525] |
ChEMBL | Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate | B | 8.47 | pKi | 3.35 | nM | Ki | J Med Chem (2008) 51: 1482-1486 [PMID:18278854] |
ChEMBL | Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins | B | 8.47 | pKi | 3.35 | nM | Ki | Eur J Med Chem (2011) 46: 5154-5161 [PMID:21899931] |
ChEMBL | Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat brain homogenate | B | 8.47 | pKi | 3.35 | nM | Ki | J Med Chem (2012) 55: 8272-8282 [PMID:22853801] |
ChEMBL | Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat liver homogenate | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2012) 55: 8272-8282 [PMID:22853801] |
ChEMBL | Binding affinity was measured on Sigma receptor type 1 with guinea pig membranes and [3H]- pentazocine as ligand. | B | 8.53 | pKi | 2.95 | nM | Ki | J Med Chem (2000) 43: 3913-3922 [PMID:11052796] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by scintillation counting | B | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem (2012) 20: 6856-6861 [PMID:23084435] |
ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222] |
ChEMBL | Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay. | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1995) 38: 2009-2017 [PMID:7783132] |
ChEMBL | Binding effinity for sigma receptor using 2 nM of [3H]-DTG as radioligand, in membranes from brain minus cerebellum | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Inhibitory activity against Sigma opioid receptor | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1991) 34: 1855-1859 [PMID:1648139] |
ChEMBL | Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1992) 35: 4516-4525 [PMID:1361578] |
ChEMBL | Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay. | B | 9.19 | pIC50 | 0.65 | nM | IC50 | J Med Chem (1995) 38: 2009-2017 [PMID:7783132] |
ChEMBL | Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine | B | 9.19 | pIC50 | 0.65 | nM | IC50 | J Med Chem (1995) 38: 1998-2008 [PMID:7783131] |
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
ChEMBL | Binding affinity to rat NET | B | 5.26 | pKi | 5500 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666] | ||||||||
ChEMBL | Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method | B | 6.41 | pKi | 391 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
Zinc finger protein 664 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105757] [UniProtKB: Q60493] | ||||||||
ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2017) 60: 2526-2551 [PMID:28218838] |
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
GtoPdb | - | - | 6.6 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542] | ||||||||
GtoPdb | - | - | 4.1 | pEC50 | - | - | - | Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978] |
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259] | ||||||||
GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Br J Pharmacol (2003) 138: 161-71 [PMID:12522086] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]