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ChEMBL ligand: CHEMBL42 (Clozapine, Clozapine (caraco), Clozapine (clozaril), Clozapine (fazaclo), Clozapine (ivax), Clozapine (mylan), Clozapine resolution mixture, Clozapine (teva), Clozapine (udl), Clozapine (versacloz), Clozaril, Fazaclo, Fazaclo odt, HF 1854, HF-1854, Leponex, NSC-757429, Versacloz, Zaponex) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278] | ||||||||
ChEMBL | Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis | B | 4.36 | pIC50 | 43300 | nM | IC50 | WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (null) |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor | B | 7.43 | pKd | 37.15 | nM | Kd | J Med Chem (1984) 27: 495-503 [PMID:6142954] |
ChEMBL | Inhibition of adrenergic alpha1A receptor (unknown origin) | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 7.72 | pKi | 19 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 8.3 | pKi | - | - | - |
Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
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 | 6.8 | pIC50 | 160 | 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 measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding. | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.82 | pKi | 15 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.42 | pIC50 | 38 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 8.2 | pKi | - | - | - |
Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
ChEMBL | Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting | B | 7.54 | pKi | 29 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting | B | 7.6 | pKi | 25 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
ChEMBL | Inhibition of rat adrenergic alpha1B receptor | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.44 | pKi | 3.59 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.19 | pIC50 | 6.49 | 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] | ||||||||
GtoPdb | - | - | 7.7 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.77 | pKi | 17 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.46 | pIC50 | 35 | 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 | Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting | B | 6.73 | pKi | 185 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 7.47 | pKi | 34 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 7.05 | pIC50 | 90 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
ChEMBL | Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting | B | 7 | pKi | 100 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding. | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha2B receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.96 | pKi | 11 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.64 | pIC50 | 23 | 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 | Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 8.94 | pKi | 1.14 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 8.1 | pIC50 | 7.88 | nM | IC50 | DrugMatrix in vitro pharmacology data |
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
ChEMBL | Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding. | B | 4.59 | pKi | 26000 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
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] |
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23] | ||||||||
ChEMBL | Binding affinity to CaM (unknown origin) by equilibrium dialysis method | B | 4.7 | pIC50 | 20000 | nM | IC50 | Eur J Med Chem (2016) 116: 36-45 [PMID:27043269] |
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157] | ||||||||
ChEMBL | Binding affinity to bovine brain CaM by FTPFACE analysis | B | 4.21 | pKd | 61000 | nM | Kd | Eur J Med Chem (2016) 116: 36-45 [PMID:27043269] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity towards human Dopamine receptor D1 | B | 6.27 | pKi | 540 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity to human cloned dopamine D1 receptor | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay | B | 6.72 | pKi | 189 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
ChEMBL | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells | B | 6.88 | pKi | 132 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034] |
ChEMBL | Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells | B | 6.88 | pKi | 132 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922] |
GtoPdb | - | - | 6.9 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells | B | 7.05 | pKi | 89 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Binding affinity against dopamine receptor D1 | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 7.28 | pKi | 53 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | F | 7.36 | pKi | 44 | nM | Ki | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
ChEMBL | Binding affinity to human dopamine D1 receptor | B | 7.36 | pKi | 44 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928] |
ChEMBL | Binding affinity against Dopamine D1 receptor | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor | B | 7.67 | pKi | 21.38 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Binding affinity to dopamine D1 receptor (unknown origin) | B | 8.12 | pKi | 7.5 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.97 | pIC50 | 107 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
ChEMBL | Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
ChEMBL | Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390 | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
ChEMBL | Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1 | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741] |
ChEMBL | In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445] |
ChEMBL | Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1 | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
ChEMBL | Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1 | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement. | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
ChEMBL | Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964] |
ChEMBL | Displacement of [3H]SCH23390 from bovine dopamine D1 receptor | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | B | 6.27 | pKi | 539 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | B | 6.45 | pKi | 354.81 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | B | 6.46 | pKi | 350 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | pKi value for Dopamine receptor D1 binding site | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
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 | 6.63 | pKi | 235 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
ChEMBL | Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain. | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane. | B | 6.77 | pKi | 169.82 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | In vitro affinity against Dopamine receptor D1 | B | 6.77 | pKi | 169.82 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue | B | 6.94 | pKi | 115 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
ChEMBL | Binding affinity against dopamine receptor D1 | B | 6.94 | pKi | 114.82 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
ChEMBL | Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand | B | 6.72 | pIC50 | 192 | nM | IC50 | J Med Chem (1989) 32: 2261-2268 [PMID:2571728] |
ChEMBL | Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain | B | 6.72 | pIC50 | 192 | nM | IC50 | J Med Chem (1990) 33: 809-814 [PMID:1967652] |
ChEMBL | Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand | B | 6.89 | pIC50 | 130 | 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 | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Binding affinity for dopamine receptor D1, activity is expressed as IC50 values. | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1995) 38: 4380-4392 [PMID:7473566] |
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 | 6.6 | pKi | 254 | 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 | 6.6 | pKi | 254 | 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 | Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression. | B | 6.06 | pKi | 876 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
ChEMBL | Displacement of [3H]N-methylspiperone from human cloned D2 dopamine receptor expressed in human fibroblasts incubated for 90 mins by scintillation counting based radioligand binding assay | B | 6.37 | pKi | 431 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
ChEMBL | Antagonist activity at human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | F | 6.41 | pKi | 389 | nM | Ki | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
ChEMBL | Binding affinity to human dopamine D2 receptor | B | 6.41 | pKi | 389 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes | B | 6.43 | pKi | 372 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 | B | 6.6 | pKi | 254 | nM | Ki | J Med Chem (1997) 40: 1-3 [PMID:9016321] |
ChEMBL | Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor | B | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | B | 6.65 | pKi | 223.87 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Displacement of [3H]spiperone human cloned dopamine D2 receptor | B | 6.65 | pKi | 223.87 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | Displacement of [3H]spiperone from human D2 receptor | B | 6.65 | pKi | 223.87 | nM | Ki | Eur J Med Chem (2014) 71: 237-249 [PMID:24316025] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | B | 6.65 | pKi | 223.87 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Binding affinity towards dopamine receptor D2 | B | 6.65 | pKi | 223.87 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay | B | 6.65 | pKi | 223.87 | nM | Ki | Medchemcomm (2011) 2: 1194-1200 |
ChEMBL | Affinity was evaluated as inhibition constant for dopamine D-2 receptor | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
ChEMBL | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
ChEMBL | Displacement of [3H]methylspiperone from human dopamine D2 receptor expressed in CHO cells | B | 6.68 | pKi | 208 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034] |
ChEMBL | Displacement of [3H]methylspiperone from dopamine D2 receptor expressed in CHO cells | B | 6.68 | pKi | 208 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922] |
ChEMBL | Binding affinity towards human D2 dopamine receptor. | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 6.72 | pKi | 190 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
ChEMBL | Binding affinity towards human Dopamine receptor D2 | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | B | 6.84 | pKi | 144 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity towards Dopamine receptor D2 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand | B | 6.86 | pKi | 138 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513] |
ChEMBL | Binding affinity towards human dopamine D2 receptor, using [3H]YM-09151 as a radioligand | B | 6.86 | pKi | 138 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512] |
ChEMBL | Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test | B | 6.87 | pKi | 134.9 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 | B | 6.87 | pKi | 6.87 | nM | pKi | J Med Chem (2004) 47: 497-508 [PMID:14736232] |
ChEMBL | Inhibition of D2 receptor (unknown origin) | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422] |
ChEMBL | Binding affinity to human cloned dopamine D2 receptor | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Binding affinity to human dopamine D2 receptor | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
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 | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.89 | pKi | 129 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 6.9 | 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]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity at human Dopamine receptor D2 by [3H]- YM 09151 displacement. | B | 6.95 | pKi | 113 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484] |
ChEMBL | Displacement of [3H]-YM 09151 from D2 receptor | B | 6.95 | pKi | 113 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562] |
ChEMBL | Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting | B | 6.97 | pKi | 106 | nM | Ki | J Med Chem (2012) 55: 1622-1634 [PMID:22243698] |
ChEMBL | Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting | B | 6.99 | pKi | 102.33 | nM | Ki | J Med Chem (2012) 55: 1622-1634 [PMID:22243698] |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay | B | 7 | pKi | >100 | nM | Ki | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
ChEMBL | Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | B | 7.04 | pKi | 91 | nM | Ki | J Med Chem (1997) 40: 4026-4029 [PMID:9406594] |
ChEMBL | Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro. | B | 7.04 | pKi | 91 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting | B | 7.05 | pKi | 89.13 | nM | Ki | Eur J Med Chem (2014) 77: 91-95 [PMID:24631727] |
ChEMBL | Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting | B | 7.05 | pKi | 88.65 | nM | Ki | Eur J Med Chem (2014) 77: 91-95 [PMID:24631727] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells | B | 7.08 | pKi | 83 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Binding affinity against Dopamine receptor D2 | B | 7.11 | pKi | 77.62 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | B | 7.13 | pKi | 74 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615] |
ChEMBL | Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Binding affinity to human dopamine D2L receptor expressed in HEK293 cells after 1 hr | B | 7.14 | pKi | 72 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
ChEMBL | Competitive antagonist activity against human dopamine D2 receptor short isoform by R-SAT assay | B | 7.14 | pKi | 72 | nM | Ki | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
ChEMBL | Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 7.15 | pKi | 71 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Binding affinity for dopamine receptor D2 determined using [3H]spiperone | B | 7.16 | pKi | 69 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting | B | 7.24 | pKi | 58.04 | nM | Ki | Eur J Med Chem (2014) 77: 91-95 [PMID:24631727] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting | B | 7.24 | pKi | 57.54 | nM | Ki | Eur J Med Chem (2014) 77: 91-95 [PMID:24631727] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells | B | 7.39 | pKi | 41 | nM | Ki | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement. | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741] |
ChEMBL | Ability to displace [3H]SCH-23390 radioligand from cloned human Dopamine receptor D2 in CHO cells | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
ChEMBL | Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
ChEMBL | Displacement of [3H]spiperone from human dopamine receptor D2(long) in CHO cell membrane | B | 7.39 | pKi | 41 | nM | Ki | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
ChEMBL | Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone | B | 7.39 | pKi | 41 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2L stably expressed in CHO cells | B | 7.41 | pKi | 39 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445] |
ChEMBL | Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2L stably expressed in Chinese hamster ovary (CHO) cells was determined. | B | 7.41 | pKi | 39 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964] |
ChEMBL | In vitro binding affinity for Dopamine receptor D2 | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544] |
ChEMBL | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2S expressed in CHO cells | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741] |
ChEMBL | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D2 in CHO cells | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
ChEMBL | Competitive binding affinity against human Dopamine receptor D2S by displacing [3H]spiperone from CHO cells | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement. | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
ChEMBL | Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2S stably expressed in Chinese hamster ovary (CHO) cells was determined. | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells | B | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
ChEMBL | Displacement of [3H]spiperone from human dopamine receptor D2(short) in CHO cell membrane | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
ChEMBL | Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) | B | 8.15 | pKi | 7.11 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.41 | pIC50 | 387 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity towards human Dopamine receptor D2 | B | 6.59 | pIC50 | 260 | 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 | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
ChEMBL | Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay | B | 6.69 | pIC50 | 206 | nM | IC50 | J Med Chem (2012) 55: 1622-1634 [PMID:22243698] |
ChEMBL | Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay | B | 6.69 | pIC50 | 204.17 | nM | IC50 | J Med Chem (2012) 55: 1622-1634 [PMID:22243698] |
ChEMBL | Antagonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as inhibition of dopamine-stimulated beta-arrestin2 recruitment measured after 20 to 22 hrs by brightglo-luciferase reporter gene assay | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
ChEMBL | Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand | B | 6.95 | pIC50 | 113 | nM | IC50 | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
ChEMBL | Inhibitory concentration against dopamine receptor D2 | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2 | B | 6.16 | pKi | 690 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
ChEMBL | Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1993) 36: 912-918 [PMID:8096548] |
ChEMBL | Inhibitory activity against dDopamine receptor D2 in calf caudate tissue, using [3H]spiperone as the radioligand | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (1989) 32: 2375-2381 [PMID:2571731] |
ChEMBL | Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168] | ||||||||
ChEMBL | Inhibition of mouse Dopamine receptor D2 | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (1996) 39: 4692-4703 [PMID:8941382] |
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 | 6.1 | pKi | 790 | nM | Ki | J Med Chem (1992) 35: 2712-2715 [PMID:1353116] |
GtoPdb | - | - | 6.2 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
ChEMBL | Binding affinity to the dopamine receptor D2L in rat brain membranes | B | 6.44 | pKi | 359 | nM | Ki | J Med Chem (1999) 42: 3342-3355 [PMID:10464021] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 6.5 | pKi | 319 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
ChEMBL | Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2 | B | 6.58 | pKi | 263.03 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473] |
ChEMBL | In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane. | B | 6.58 | pKi | 263.03 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Affinity against Dopamine receptor D2 | B | 6.58 | pKi | 263.03 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | pKi value for Dopamine receptor D2 binding site | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
ChEMBL | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
ChEMBL | Inhibition of [3H]spiperone binding to rat dopamine D2 receptor | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Displacement of [3H]-N-methylspiperone from rat recombinant dopamine D2 short receptor expressed in CHO cells | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement. | B | 6.77 | pKi | 168 | nM | Ki | J Med Chem (1993) 36: 3073-3076 [PMID:7901415] |
ChEMBL | Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting | B | 6.81 | pKi | 155 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Binding affinity at dopamine D2 receptor in rat striatal membranes | B | 6.84 | pKi | 144.54 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534] |
ChEMBL | Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting | B | 6.85 | pKi | 140 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
ChEMBL | Binding affinity of [3H]spiperone towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain | B | 6.86 | pKi | 138 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting | B | 6.88 | pKi | 130.7 | nM | Ki | Eur J Med Chem (2014) 74: 427-439 [PMID:24487191] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum | B | 6.88 | pKi | 130.7 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum tissue after 20 mins by scintillation counting | B | 6.89 | pKi | 130 | nM | Ki | Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515] |
ChEMBL | Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting | B | 6.89 | pKi | 130 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis | B | 6.89 | pKi | 128.7 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
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 113 to 362 | B | 6.93 | pKi | 118 | 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 | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1327-1330 |
ChEMBL | Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 913-918 |
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 | 7.03 | pKi | 93 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 7.08 | pKi | 83.18 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
ChEMBL | Binding affinity against Dopamine receptor D2 from rat striatum | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (1998) 41: 1997-2009 [PMID:9622541] |
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 | 7.19 | pKi | 64.2 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
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 | 7.2 | pKi | 63.1 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain | B | 7.26 | pKi | 55 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | B | 7.27 | pKi | 53.6 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | B | 7.27 | pKi | 53.6 | nM | Ki | J Med Chem (1995) 38: 4211-4222 [PMID:7473548] |
ChEMBL | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | B | 7.27 | pKi | 53.6 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
ChEMBL | Binding affinity against dopamine D2 receptor | B | 7.34 | pKi | 45.71 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
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 | 7.47 | pKi | 34 | 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 | 7.47 | pKi | 34 | nM | Ki | J Med Chem (1987) 30: 1100-1105 [PMID:2884314] |
ChEMBL | Binding activity against dopamine D2 receptor in rat brain, using [3H]spiperone as the radioligand | B | 5.56 | pIC50 | 2770 | nM | IC50 | J Med Chem (1989) 32: 2261-2268 [PMID:2571728] |
ChEMBL | Binding affinity for Dopamine receptor D2 using [3H]spiperone in rat brain | B | 5.56 | pIC50 | 2770 | nM | IC50 | J Med Chem (1990) 33: 809-814 [PMID:1967652] |
ChEMBL | In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand | B | 5.68 | pIC50 | 2108 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
ChEMBL | In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum | B | 5.79 | pIC50 | 1610 | nM | IC50 | J Med Chem (1994) 37: 2308-2314 [PMID:7914536] |
ChEMBL | Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand | B | 5.79 | pIC50 | 1610 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue | B | 6 | pIC50 | 1000 | 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 | 6.08 | pIC50 | 830 | nM | IC50 | J Med Chem (1995) 38: 1119-1131 [PMID:7707315] |
ChEMBL | In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2 | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (1992) 35: 4516-4525 [PMID:1361578] |
ChEMBL | Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (1986) 29: 359-369 [PMID:2869146] |
ChEMBL | Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (1989) 32: 1147-1156 [PMID:2542551] |
ChEMBL | Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2 | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (1992) 35: 1092-1101 [PMID:1348090] |
ChEMBL | Ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat corpus striatum | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1988) 31: 618-624 [PMID:2894466] |
ChEMBL | Binding affinity against dopamine receptor D2 | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (1995) 38: 4380-4392 [PMID:7473566] |
ChEMBL | Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats | B | 6.54 | pIC50 | 290 | 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 | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (1996) 39: 149-157 [PMID:8568802] |
ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D2 from striatum of the rat brain | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (1989) 32: 2573-2582 [PMID:2573732] |
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 | 6.76 | pIC50 | 172 | nM | IC50 | J Med Chem (1991) 34: 1860-1866 [PMID:1676427] |
ChEMBL | Inhibition of spiropiperidone binding at dopamine receptor D2 of rat. | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2001) 44: 372-389 [PMID:11462978] |
ChEMBL | Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes. | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (1987) 30: 1807-1812 [PMID:2888897] |
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 | 6.33 | pKi | 466 | 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 | Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Competitive binding affinity against human Dopamine receptor D3 by displacing [3H]spiperone from CHO cells | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741] |
ChEMBL | In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445] |
ChEMBL | Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3 | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement. | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
ChEMBL | Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membrane | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
ChEMBL | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D3 in CHO cells | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
ChEMBL | Ability to displace [3H]spiperone from the cloned human D3 dopamine receptor stably expressed in Chinese hamster ovary (CHO) cells was determined. | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor | B | 6.04 | pKi | 912.01 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Displacement of [3H]N-methylspiperone from human cloned D3 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay | B | 6.19 | pKi | 646 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
ChEMBL | Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding. | B | 6.29 | pKi | 513 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
GtoPdb | - | - | 6.3 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163] |
ChEMBL | Binding affinity on human Dopamine receptor D3 expressed in CHO cells using radioligand [3H]-YM 09151 | B | 6.34 | pKi | 454 | nM | Ki | J Med Chem (1997) 40: 1-3 [PMID:9016321] |
ChEMBL | Binding affinity to dopamine D3 receptor | B | 6.43 | pKi | 372.3 | nM | Ki | J Nat Prod (2010) 73: 1015-1021 [PMID:20408551] |
ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 6.44 | pKi | 360 | 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 | 6.5 | pKi | 319 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
ChEMBL | Binding affinity to dopamine D3 receptor (unknown origin) | B | 6.5 | pKi | 319 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
ChEMBL | Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry | B | 6.5 | pKi | 319 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 6.53 | pKi | 295 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Binding affinity towards human dopamine receptor D3 | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | B | 6.62 | pKi | 242 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity to human cloned dopamine D3 receptor | B | 6.62 | pKi | 240 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
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 | 6.62 | pKi | 240 | 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 | 6.62 | pKi | 6.62 | nM | pKi | J Med Chem (2004) 47: 497-508 [PMID:14736232] |
ChEMBL | Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test | B | 6.62 | pKi | 239.88 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | B | 6.65 | pKi | 222 | 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 | 6.65 | pKi | 222 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D3 stably expressed in HEK393 cell lines | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | B | 6.7 | pKi | 200 | 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 | 6.7 | pKi | 200 | 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 | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in HEK293 cells | B | 6.7 | pKi | 200 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.06 | pKi | 88 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | B | 7.06 | pKi | 88 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.59 | pIC50 | 258 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
GtoPdb | - | - | 5.7 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
ChEMBL | Binding affinity towards baculovirus expressed rat dopamine D3 receptors | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
ChEMBL | Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle | B | 6.47 | pKi | 340.1 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | B | 6.49 | pKi | 320 | 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 | 6.5 | pKi | 319 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting | B | 6.58 | pKi | 260.1 | nM | Ki | Eur J Med Chem (2014) 74: 427-439 [PMID:24487191] |
ChEMBL | Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis | B | 6.62 | pKi | 239.8 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
ChEMBL | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
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 | 6.73 | pKi | 188 | 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 | 6.79 | pKi | 161 | nM | Ki | Med Chem Res (2004) 13: 25-33 |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand | B | 5.05 | pKi | 9000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513] |
ChEMBL | Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor | B | 7.14 | pKi | 72 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
ChEMBL | Displacement of [3H]-YM 09151 from human Dopamine receptor D4 | B | 7.15 | pKi | 71 | nM | Ki | J Med Chem (1995) 38: 4950-4952 [PMID:8523409] |
ChEMBL | Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (1997) 40: 1-3 [PMID:9016321] |
ChEMBL | Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting | B | 7.22 | pKi | 60 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
ChEMBL | Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting | B | 7.22 | pKi | 60 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
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 | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | Binding affinity to human cloned dopamine D4 receptor | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 | B | 7.27 | pKi | 7.27 | 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 | 7.27 | pKi | 53.7 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778] |
ChEMBL | In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 7.33 | pKi | 47 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
ChEMBL | Displacement of radiolabeled clozapine from human dopamine D4.4 receptor | B | 7.36 | pKi | 44 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Binding affinity towards human dopamine-4.2 receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity towards human dopamine receptor D4 | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Inhibition of human dopamine D4 receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay | B | 7.41 | pKi | 39 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
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 | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
GtoPdb | - | - | 7.5 | pKi | - | - | - | Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973] |
ChEMBL | In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4 | B | 7.52 | pKi | 30.4 | 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 | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
ChEMBL | Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2002) 45: 5727-5735 [PMID:12477356] |
ChEMBL | Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
ChEMBL | In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 | B | 7.55 | pKi | 28.4 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206] |
ChEMBL | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
ChEMBL | Affinity was evaluated as inhibition constant for dopamine D-4 receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
ChEMBL | Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | Displacement of [3H]-YM 09151 from D4 receptor | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562] |
ChEMBL | Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement. | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484] |
ChEMBL | Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
ChEMBL | Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells | B | 7.77 | pKi | 17 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
ChEMBL | Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1997) 40: 2688-2693 [PMID:9276014] |
ChEMBL | Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4 | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
ChEMBL | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
ChEMBL | Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
ChEMBL | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445] |
ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741] |
ChEMBL | Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
ChEMBL | Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1997) 40: 4026-4029 [PMID:9406594] |
ChEMBL | Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964] |
ChEMBL | In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement. | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
ChEMBL | In vitro binding affinity for Dopamine receptor D4 | B | 7.8 | pKi | 15.85 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544] |
ChEMBL | Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells | B | 7.8 | pKi | 7.8 | D4 | Log Ki | J Med Chem (2001) 44: 1151-1157 [PMID:11312915] |
ChEMBL | Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay | B | 7.82 | pKi | 15 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1327-1330 |
ChEMBL | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Binding affinity towards human Dopamine receptor D4.2 in CHO cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Inhibition of human dopamine D4 receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
ChEMBL | compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615] |
ChEMBL | Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand | B | 8.05 | pKi | 9 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512] |
ChEMBL | Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation | F | 6.77 | pIC50 | 168 | nM | IC50 | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
ChEMBL | Percent inhibition against Dopamine receptor D4 at 1 uM | B | 6.81 | pIC50 | 156 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
ChEMBL | Inhibitory concentration against dopamine receptor D4 | B | 6.86 | pIC50 | 138 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
ChEMBL | Inhibition of human dopamine D4.4 receptor | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
ChEMBL | Displacement of radiolabeled clozapine from human dopamine D4.4 receptor | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Binding affinity towards human D4.2 receptor | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
ChEMBL | Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells | B | 7.39 | pIC50 | 41 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
ChEMBL | Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
ChEMBL | In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement. | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
ChEMBL | Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2000) 43: 3923-3932 [PMID:11052797] |
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
ChEMBL | Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain. | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay | B | 6.11 | pKi | 780 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
GtoPdb | - | - | 6.6 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL | Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay | B | 6.63 | pKi | 235 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells | B | 6.7 | pKi | 198 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
ChEMBL | Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1986) 29: 359-369 [PMID:2869146] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method | B | 4.77 | pKi | 17000 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Binding affinity to human ERG expressed in HEK293 cells | B | 4.77 | pKi | 17000 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.06 | pKi | 8660.6 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay | B | 5.39 | pKi | 4060 | nM | Ki | J Med Chem (2007) 50: 2931-2941 [PMID:17536794] |
ChEMBL | Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA | B | 5.51 | pKi | 3080 | nM | Ki | J Med Chem (2007) 50: 2931-2941 [PMID:17536794] |
ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.98 | pIC50 | 10571 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | F | 5.24 | pIC50 | 5754.4 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Inhibition of human ERG | B | 5.4 | pIC50 | 3981.07 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
ChEMBL | Inhibition of human ERG | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928] |
ChEMBL | Inhibition of human ERG | B | 6.05 | pIC50 | 901 | nM | IC50 | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay | B | 6.19 | pIC50 | 650 | nM | IC50 | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 6.49 | pIC50 | 323.59 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 6.49 | pIC50 | 323.59 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 6.49 | pIC50 | 323.59 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human ERG channel | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
ChEMBL | Inhibition of human ERG channel | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 6.72 | pIC50 | 191 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 6.72 | pIC50 | 190.55 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Binding affinity to human histamine H1 receptor | B | 8.51 | pKd | 3.1 | nM | Kd | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
ChEMBL | Binding affinity against histamine H1 receptor | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells | B | 8.62 | pKi | 2.38 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Binding affinity towards human histamine H1 receptor | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity to human cloned histamine H1 receptor | B | 8.74 | pKi | 1.8 | 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 | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230] |
ChEMBL | Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Inhibition of histamine H1 receptor (unknown origin) | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 9.24 | pKi | 0.57 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 9.6 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 8.31 | pIC50 | 4.91 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inverse agonist activity at human histamine H1 receptor by R-SAT assay | B | 9.4 | pEC50 | 0.4 | nM | EC50 | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
ChEMBL | Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay. | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand | B | 7.64 | pIC50 | 23 | 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 | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Displacement of [3H]mepyramine from H1R in rat brain | B | 8.05 | pIC50 | 9 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666] |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting | B | 7.91 | pKi | 12.2 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum | B | 8.09 | pKi | 8.1 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting | B | 8.17 | pKi | 6.8 | nM | Ki | Eur J Med Chem (2014) 74: 427-439 [PMID:24487191] |
ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
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 | 5.45 | pKi | 3550 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.44 | pIC50 | 3610 | nM | IC50 | DrugMatrix in vitro pharmacology data |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Antagonist potency against human H3 receptor in GTPgamma-S-Assay | F | 6.2 | pKi | 631 | nM | Ki | J Med Chem (2005) 48: 306-311 [PMID:15634025] |
H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
GtoPdb | - | - | 5.8 | pKi | - | - | - | J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375] |
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM | B | 7.15 | pKd | 70.2 | nM | Kd | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM | B | 7.68 | pKd | 20.9 | nM | Kd | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
ChEMBL | Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM | B | 7.84 | pKd | 14.5 | nM | Kd | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells | B | 7.92 | pKd | 11.9 | nM | Kd | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
ChEMBL | Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis | B | 6.3 | pKi | 501.19 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
GtoPdb | - | - | 6.7 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells | B | 6.75 | pKi | 177.83 | nM | Ki | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
GtoPdb | - | - | 5.5 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
GtoPdb | - | - | 5.7 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
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 | 9 | pKi | 1 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Binding affinity to M1 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.61 | pKi | 2.47 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to human cloned muscarinic M1 receptor | B | 8.74 | pKi | 1.8 | 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 | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230] |
ChEMBL | Binding affinity towards human M1 muscarinic receptor. | B | 9.01 | pKi | 0.98 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
GtoPdb | - | - | 7.9 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2003) 100: 13674-9 [PMID:14595031] |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8 | pIC50 | 10 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 8.03 | pIC50 | 9.4 | 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 | 8.03 | pIC50 | 9.4 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
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 | 7.26 | pKi | 55 | 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 | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by radioligand [3H]pirenzepine binding assay. | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
GtoPdb | - | - | 7.7 | pIC50 | - | - | - | Mol Pharmacol (2006) 70: 1974-83 [PMID:16959945] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.77 | pKi | 169 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to M2 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.32 | pIC50 | 476 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Agonist activity at muscarinic M2 receptor (unknown origin) expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
ChEMBL | Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by Radio ligand [3H]quinuclidinyl binding assay. | B | 7.34 | pKi | 46 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Binding affinity to M3 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.77 | pKi | 17 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.11 | pIC50 | 78 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Binding affinity to M4 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.2 | pKi | 6.3 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.35 | pIC50 | 45 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Agonist activity at muscarinic M4 receptor (unknown origin) expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Binding affinity to M5 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.02 | pKi | 9.53 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.89 | pIC50 | 13 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.84 | pKi | 1458 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.83 | pIC50 | 1470 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
ChEMBL | Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter | B | 6.16 | pKi | 697 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 | pIC50 | 10000 | 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 | 5.1 | pIC50 | 7943.28 | 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 | 5.1 | pIC50 | 7943.28 | 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 | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 1 receptor | B | 6.15 | pKi | 710 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Binding affinity against 5-Hydroxytryptamine 1A receptor | B | 6.38 | pKi | 416.87 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand | B | 6.57 | pKi | 270 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728] |
ChEMBL | Binding affinity to 5HT1A receptor (unknown origin) | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr | B | 6.84 | pKi | 143 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 6.84 | pKi | 143 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr | B | 6.84 | pKi | 143 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101] |
ChEMBL | Binding affinity to human cloned 5HT1A receptor | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Inhibition of human 5HT1A receptor | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
GtoPdb | - | - | 6.9 | pKi | - | - | - |
Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 7 | pKi | 101 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity to human 5HT1A receptor | B | 8.05 | pKi | 8.9 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
ChEMBL | Binding affinity to 5-HT1A receptor (unknown origin) | B | 8.2 | pKi | 6.38 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
ChEMBL | Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
ChEMBL | Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice. | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1996) 39: 4692-4703 [PMID:8941382] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
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 | 6.19 | pKi | 640 | 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 | 6.35 | pKi | 443 | nM | Ki | J Med Chem (2000) 43: 270-277 [PMID:10649982] |
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 | 6.38 | pKi | 415 | nM | Ki | J Med Chem (1999) 42: 3342-3355 [PMID:10464021] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate | B | 6.42 | pKi | 380 | nM | Ki | Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.55 | pKi | 281 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting | B | 6.59 | pKi | 260 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting | B | 6.59 | pKi | 260 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
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 | 6.61 | pKi | 247 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat brain cortex | B | 6.73 | pKi | 185.6 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting | B | 6.73 | pKi | 185.6 | nM | Ki | Eur J Med Chem (2014) 74: 427-439 [PMID:24487191] |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | B | 6.79 | pKi | 161 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A receptor in rat CRL:CD(SD)BR-COBS hippocampus by scintillation spectrometry | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
ChEMBL | Binding affinity of [3H]-8-OH-DPAT towards 5-hydroxytryptamine 1A receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain. | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (1996) 39: 2435-2437 [PMID:8691438] |
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis | B | 6.85 | pKi | 141.6 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
ChEMBL | Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting | B | 6.85 | pKi | 140 | nM | Ki | Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515] |
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 | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations | B | 6.95 | pKi | 111 | nM | Ki | J Med Chem (1994) 37: 1060-1062 [PMID:7909336] |
ChEMBL | Compound was evaluated for its binding affinity against 5-hydroxytryptamine 1A receptor from rat cerebral cortex | B | 6.95 | pKi | 111 | nM | Ki | J Med Chem (1998) 41: 1997-2009 [PMID:9622541] |
ChEMBL | Binding affinity at 5HT1A receptor in rat striatal membranes | B | 7.02 | pKi | 95.5 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534] |
ChEMBL | Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101 | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (1995) 38: 4198-4210 [PMID:7473547] |
ChEMBL | The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101. | B | 7.41 | pKi | 38.5 | nM | Ki | J Med Chem (1995) 38: 4211-4222 [PMID:7473548] |
ChEMBL | In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin | B | 5.7 | pIC50 | 2000 | 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 | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1996) 39: 149-157 [PMID:8568802] |
ChEMBL | In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus | B | 5.99 | pIC50 | 1015.5 | nM | IC50 | J Med Chem (1994) 37: 2308-2314 [PMID:7914536] |
ChEMBL | Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand | B | 6 | pIC50 | 1010 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand. | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1991) 34: 1860-1866 [PMID:1676427] |
ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (1991) 34: 1068-1072 [PMID:1672156] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.31 | pIC50 | 491 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand | B | 6.57 | pIC50 | 267.6 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 6.2 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.02 | pKi | 959 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 5.68 | pIC50 | 2109 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay | B | 6 | pKi | >1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 6.4 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT1E receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 6.4 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Binding affinity to human 5HT2A receptor | B | 6.64 | pKi | 230 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 7.44 | pKi | 36.31 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membranes by radioligand binding assay | B | 7.74 | pKi | 18 | nM | Ki | J Nat Prod (2015) 78: 722-729 [PMID:25695425] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method | B | 7.79 | pKi | 16.1 | nM | Ki | Medchemcomm (2018) 9: 1069-1075 [PMID:30108996] |
ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor measured after 90 mins by microbeta scintillation counting method | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3216-3219 [PMID:27261181] |
ChEMBL | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method | B | 7.82 | pKi | 15 | nM | Ki | Medchemcomm (2015) 6: 601-605 |
ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method | B | 7.89 | pKi | 13 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity to 5HT2A receptor (unknown origin) | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 8.02 | pKi | 9.6 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Displacement of [125]DOI from human recombinant full length 5HT2A receptor expressed in HEK293E cells | B | 8.02 | pKi | 9.6 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor | B | 8.04 | pKi | 9.12 | nM | Ki | Eur J Med Chem (2014) 71: 237-249 [PMID:24316025] |
ChEMBL | Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor | B | 8.04 | pKi | 9.12 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor | B | 8.04 | pKi | 9.12 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | B | 8.04 | pKi | 9.12 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | B | 8.04 | pKi | 9.12 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.04 | pKi | 9.12 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay | B | 8.04 | pKi | 9.12 | nM | Ki | Medchemcomm (2011) 2: 1194-1200 |
ChEMBL | Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Binding affinity to human cloned 5HT2A receptor | B | 8.05 | pKi | 8.9 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Binding affinity to 5-HT2A receptor (unknown origin) | B | 8.07 | pKi | 8.57 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) | B | 8.13 | pKi | 7.41 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) | B | 8.14 | pKi | 7.3 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Antagonist activity at 5HT2A receptor (unknown origin) | B | 8.27 | pKi | 5.35 | nM | Ki | Eur J Med Chem (2020) 193: 112214-112214 [PMID:32182489] |
ChEMBL | Binding affinity to 5-HT2A receptor (unknown origin) | B | 8.27 | pKi | 5.35 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity towards human 5-HT2A receptor in BEK cells | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 8.32 | pKi | 4.84 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2A receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Binding affinity to human 5HT2A receptor | B | 8.52 | pKi | 3.03 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
ChEMBL | Displacement of [3H]-Ketanserin from 5-HT2A receptor (unknown origin) incubated for 90 mins by microbeta counting method | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Binding affinity against 5-Hydroxytryptamine 2A receptor | B | 8.57 | pKi | 2.69 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Binding affinity to human 5HT2A receptor | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 8.92 | pKi | 1.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 9 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927] |
ChEMBL | Inhibitory concentration against human 5-HT2A receptor in BEK cells | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1996) 39: 4044-4057 [PMID:8831770] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 8.38 | pIC50 | 4.2 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 8.52 | pIC50 | 3 | 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 | Compound was tested for Antagonistic activity against denuded rat aorta | F | 8.62 | pKd | 2.4 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473] |
ChEMBL | Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta | F | 9.16 | pKd | 0.69 | nM | Kd | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
ChEMBL | In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor | B | 7.56 | pKi | 27.54 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting | B | 7.68 | pKi | 21 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
ChEMBL | Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay. | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor | B | 7.82 | pKi | 15.14 | nM | Ki | J Med Chem (1996) 39: 143-148 [PMID:8568801] |
ChEMBL | Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | B | 7.84 | pKi | 14.5 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652] |
ChEMBL | Binding affinity at 5HT2A receptor in rat striatal membranes | B | 7.88 | pKi | 13.18 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534] |
ChEMBL | Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting | B | 7.89 | pKi | 12.9 | nM | Ki | Eur J Med Chem (2014) 74: 427-439 [PMID:24487191] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex | B | 7.89 | pKi | 12.9 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis | B | 7.94 | pKi | 11.6 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2010) 53: 4803-4807 [PMID:20481570] |
ChEMBL | Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | nM | Ki | J Med Chem (2009) 52: 151-169 [PMID:19072656] |
ChEMBL | Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2002) 45: 344-359 [PMID:11784139] |
ChEMBL | Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2005) 48: 1705-1708 [PMID:15771414] |
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 | 8.03 | pKi | 9.4 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
ChEMBL | Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting | B | 8.05 | pKi | 8.9 | nM | Ki | Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515] |
ChEMBL | Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor. | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
ChEMBL | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2A receptor | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
ChEMBL | Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor) | B | 8.12 | pKi | 7.59 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473] |
ChEMBL | Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex | B | 8.12 | pKi | 7.59 | 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 | 8.17 | pKi | 6.7 | nM | Ki | J Med Chem (2002) 45: 5136-5149 [PMID:12408724] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membrane | B | 8.22 | pKi | 6.05 | nM | Ki | Eur J Med Chem (2009) 44: 800-808 [PMID:18603331] |
ChEMBL | Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 913-918 |
ChEMBL | In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane. | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Affinity at 5-hydroxytryptamine 2A receptor of the rat brain cortex was assessed on the basis of their ability to displace [3H]ketanserin | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (2000) 43: 1901-1909 [PMID:10821703] |
GtoPdb | - | - | 8.9 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845] |
ChEMBL | In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex | B | 7.14 | pIC50 | 72 | 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 | 7.39 | pIC50 | 40.7 | 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 | 7.89 | pIC50 | 13 | 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 | 7.92 | pIC50 | 12 | 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 | 8.11 | pIC50 | 7.8 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
ChEMBL | Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values. | B | 8.11 | pIC50 | 7.8 | nM | IC50 | J Med Chem (1995) 38: 4380-4392 [PMID:7473566] |
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 | 8.14 | pKi | 7.18 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
GtoPdb | - | - | 8.8 | pKi | - | - | - |
J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; 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 | 7.96 | pIC50 | 11 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inverse agonist activity at human 5HT2B receptor by R-SAT assay | B | 7.7 | pEC50 | 20 | nM | EC50 | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
ChEMBL | Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus | F | 6.77 | pKd | 169.82 | nM | Kd | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
ChEMBL | Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor | F | 6.9 | pKd | 125.89 | nM | Kd | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 7.14 | pKi | 72.44 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | B | 7.62 | pKi | 24 | nM | Ki | Eur J Med Chem (2013) 62: 214-221 [PMID:23353740] |
ChEMBL | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | B | 7.64 | pKi | 23 | nM | Ki | Eur J Med Chem (2013) 66: 122-134 [PMID:23792350] |
ChEMBL | Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity to human cloned 5HT2C receptor | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus. | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (1999) 42: 2774-2797 [PMID:10425088] |
ChEMBL | Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2002) 45: 54-71 [PMID:11754579] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507] |
ChEMBL | Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. | B | 7.89 | pKi | 13 | nM | Ki | US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013) |
ChEMBL | Displacement of [125]DOI from human recombinant full length 5HT2C receptor expressed in HEK293E cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2014) 57: 2670-2682 [PMID:24559051] |
ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Displacement of [3H]mesulergine from human cloned 5HT2C receptor | B | 7.98 | pKi | 10.47 | nM | Ki | J Med Chem (2008) 51: 6085-6094 [PMID:18783204] |
ChEMBL | Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor | B | 7.98 | pKi | 10.47 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor | B | 7.98 | pKi | 10.47 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944] |
ChEMBL | Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor | B | 7.98 | pKi | 10.47 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 8.03 | pKi | 9.33 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2000) 43: 4678-4693 [PMID:11101359] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 2C receptor | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Binding affinity to 5HT2C receptor (unknown origin) | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2014) 57: 9578-9597 [PMID:25343529] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.5 | pKi | 3.16 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity against 5-Hydroxytryptamine 2C receptor | B | 8.54 | pKi | 2.88 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Binding affinity to 5-HT2C receptor (unknown origin) | B | 8.54 | pKi | 2.88 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
GtoPdb | - | - | 8.7 | pKi | - | - | - |
J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]; J Neurochem (1999) 72: 2127-34 [PMID:10217294] |
ChEMBL | Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 2010-2018 [PMID:9622542] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.22 | pIC50 | 6.04 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inverse agonist activity at human 5HT2C receptor by R-SAT assay | B | 6.6 | pEC50 | 250 | nM | EC50 | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
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 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | B | 7.38 | pKi | 41.9 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex | B | 7.48 | pKi | 33.1 | nM | Ki | Medchemcomm (2015) 6: 831-838 |
ChEMBL | Compound was evaluated for its binding affinity towards rat r5-hydroxytryptamine 2C receptor | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis | B | 7.79 | pKi | 16.2 | nM | Ki | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
ChEMBL | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
ChEMBL | Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2C serotonin receptor. | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
ChEMBL | Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand | B | 7.96 | pIC50 | 11 | 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 | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1997) 40: 4146-4153 [PMID:9406603] |
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
ChEMBL | Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
ChEMBL | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT3 receptor (unknown origin) by PDSP assay | B | 6 | pKi | 1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity against 5-Hydroxytryptamine 3 receptor | B | 6.73 | pKi | 186.21 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
ChEMBL | Binding affinity to 5-HT3 receptor (unknown origin) | B | 6.73 | pKi | 186.21 | nM | Ki | Med Chem Res (2013) 22: 520-530 |
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 | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay | B | 6 | pKi | >1000 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
GtoPdb | - | - | 6.5 | pKi | - | - | - |
FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
GtoPdb | - | - | 5.3 | pKi | - | - | - | Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2012) 55: 5704-5719 [PMID:22537153] |
ChEMBL | Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507] |
ChEMBL | Binding affinity to human cloned 5HT6 receptor | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
ChEMBL | Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation | F | 8 | pKi | <10 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
GtoPdb | - | - | 8.1 | pKi | - | - | - |
J Neurochem (1996) 66: 47-56 [PMID:8522988]; Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]; Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]; Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958] |
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) | B | 8.21 | pKi | 6.1 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) | B | 8.22 | pKi | 6.03 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 8.3 | pKi | 5.05 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand | B | 8.32 | pKi | 4.8 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2295-2299 [PMID:11055342] |
ChEMBL | Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101] |
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 | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay | F | 7.69 | pIC50 | 20.3 | nM | IC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
ChEMBL | Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 10017-10039 [PMID:30383372] |
ChEMBL | Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2014) 22: 1782-1790 [PMID:24495863] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 7.96 | pIC50 | 11 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 8.4 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]; J Neurochem (1998) 71: 2169-77 [PMID:9798944]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630] |
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-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2018) 145: 790-804 [PMID:29407591] |
ChEMBL | Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay | B | 7 | pKi | 100 | nM | Ki | Medchemcomm (2012) 3: 580-583 |
ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method | B | 7.32 | pKi | 48.4 | nM | Ki | Eur J Med Chem (2019) 179: 1-15 [PMID:31229883] |
ChEMBL | Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor | B | 7.32 | pKi | 48 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method | B | 7.32 | pKi | 47.86 | nM | Ki | Eur J Med Chem (2019) 179: 1-15 [PMID:31229883] |
ChEMBL | Displacement of [3H]-5-CT from human recombinant 5-HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method | B | 7.32 | pKi | 47.4 | nM | Ki | Eur J Med Chem (2019) 170: 261-275 [PMID:30904783] |
ChEMBL | Displacement of [3H]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | B | 7.34 | pKi | 45.5 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
ChEMBL | Displacement of [3H]-5-CT from 5-HT7b receptor (unknown origin) | B | 7.34 | pKi | 45.5 | nM | Ki | ACS Med Chem Lett (2017) 8: 390-394 [PMID:28435524] |
ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Displacement of [3H]5CT from 5HT7 receptor | B | 7.4 | pKi | 39.81 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2465-2468 [PMID:20346662] |
ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cell membranes by radioligand binding assay | B | 7.43 | pKi | 37 | nM | Ki | J Nat Prod (2015) 78: 722-729 [PMID:25695425] |
ChEMBL | Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis | B | 7.6 | pKi | 25 | nM | Ki | Eur J Med Chem (2014) 78: 324-339 [PMID:24691057] |
ChEMBL | Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2020) 201: 112437-112437 [PMID:32673902] |
ChEMBL | Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
ChEMBL | Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101] |
ChEMBL | Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2015) 23: 212-221 [PMID:25435254] |
ChEMBL | Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2016) 112: 258-269 [PMID:26900658] |
ChEMBL | Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2018) 147: 102-114 [PMID:29425815] |
ChEMBL | Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 7.74 | pKi | 18 | nM | Ki | Medchemcomm (2018) 9: 1033-1044 [PMID:30108992] |
ChEMBL | Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2019) 178: 740-751 [PMID:31229876] |
ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
ChEMBL | Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | B | 7.74 | pKi | 18 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
GtoPdb | - | - | 7.8 | pKi | - | - | - |
Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804] |
ChEMBL | Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
ChEMBL | Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method | B | 7.94 | pKi | 11.4 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) | B | 8.23 | pKi | 5.89 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) | B | 8.26 | pKi | 5.5 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
GtoPdb | - | - | 7.4 | 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 | Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting | B | 7.2 | pKi | 62.6 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 7 receptor | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226] |
GtoPdb | - | - | 8.2 | pKi | - | - | - |
Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Binding affinity to human SERT | B | 5.41 | pKi | 3900 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
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 | 6.54 | pKi | 290 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of 5-HT uptake at SERT (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Med Chem Res (2013) 22: 520-530 |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 6.26 | pIC50 | 546 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
ChEMBL | Inhibitory concentration against reuptake of 5-HT from rat synaptosomes | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
ChEMBL | Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain | B | 5.07 | pKi | 8500 | nM | Ki | J Med Chem (1998) 41: 1557-1560 [PMID:9572880] |
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 | 5.07 | pKi | 8500 | nM | Ki | J Med Chem (1998) 41: 5402-5409 [PMID:9876110] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
ChEMBL | Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1992) 35: 4516-4525 [PMID:1361578] |
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
ChEMBL | Binding affinity to rat NET | B | 6.41 | pKi | 390 | nM | Ki | Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716] |
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
GtoPdb | - | - | 6.9 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542] | ||||||||
GtoPdb | - | - | 3.8 | pEC50 | - | - | - | Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978] |
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]