apomorphine [Ligand Id: 33] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL53 (6a.beta.-aporphine-10,11-diol, APL-130277, Apomorphine, Apomorphinum, VR-040, VR040) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells | B | 6.17 | pKd | 680 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells | B | 6.18 | pKi | 660 | nM | Ki | Eur J Med Chem (2012) 55: 255-261 [PMID:22846798] |
| ChEMBL | Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assay | B | 6.19 | pKi | 650 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
Nature (1991) 350: 614-9 [PMID:1826762]; J Biol Chem (1994) 269: 27925-31 [PMID:7525564] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis | B | 6.31 | pKi | 492 | nM | Ki | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay | B | 6.43 | pKi | 372 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| ChEMBL | Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem (2008) 16: 6675-6681 [PMID:18562201] |
| ChEMBL | Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter | B | 7.14 | pKi | 72 | nM | Ki | Eur J Med Chem (2011) 46: 2992-2999 [PMID:21550699] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting | B | 7.14 | pKi | 72 | nM | Ki | Bioorg Med Chem (2009) 17: 4756-4762 [PMID:19454369] |
| ChEMBL | Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assay | B | 8.34 | pKi | 4.6 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 6.28 | pEC50 | 520.8 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 6.3 | pEC50 | 501.19 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production | F | 7.28 | pEC50 | 52 | nM | EC50 | Bioorg Med Chem (2008) 16: 3438-3444 [PMID:18313303] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins | F | 7.59 | pEC50 | 25.7 | nM | EC50 | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.4 | pEC50 | 3.98 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.42 | pEC50 | 3.77 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells | B | 7 | pKi | 101 | nM | Ki | Bioorg Med Chem (2008) 16: 4563-4568 [PMID:18313931] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum | B | 6 | pKi | 1010 | nM | Ki | J Med Chem (2008) 51: 983-987 [PMID:18251489] |
| ChEMBL | In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate | B | 6.05 | pKi | 888 | nM | Ki | J Med Chem (1989) 32: 1431-1435 [PMID:2525621] |
| ChEMBL | In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1 | B | 6.63 | pKi | 236 | nM | Ki | J Med Chem (1996) 39: 3503-3513 [PMID:8784448] |
| ChEMBL | In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement. | B | 6.63 | pKi | 236 | nM | Ki | J Med Chem (1996) 39: 3491-3502 [PMID:8784447] |
| ChEMBL | Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1 | B | 6.63 | pKi | 236 | nM | Ki | J Med Chem (1995) 38: 647-658 [PMID:7861413] |
| ChEMBL | Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand | B | 6.63 | pKi | 236 | nM | Ki | J Med Chem (1990) 33: 1800-1805 [PMID:1971309] |
| ChEMBL | Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand | B | 6.66 | pKi | >221 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
| ChEMBL | Displacement of [3H]SCH-23390 from rat dopamine D1 receptor | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2007) 50: 171-181 [PMID:17228858] |
| ChEMBL | Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand. | B | 6.74 | pKi | 181.97 | nM | Ki | J Med Chem (2000) 43: 599-608 [PMID:10691686] |
| ChEMBL | Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (1986) 29: 1904-1912 [PMID:3761310] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1990) 33: 2408-2412 [PMID:1975274] |
| ChEMBL | Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane | B | 6.35 | pIC50 | 444 | nM | IC50 | J Med Chem (1990) 33: 3122-3124 [PMID:2147956] |
| ChEMBL | In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement. | B | 6.36 | pIC50 | 432 | nM | IC50 | J Med Chem (1990) 33: 600-607 [PMID:2405158] |
| ChEMBL | Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes | B | 6.37 | pIC50 | 430 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 883-886 [PMID:11294383] |
| ChEMBL | Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined | B | 6.42 | pIC50 | 384 | nM | IC50 | J Med Chem (1990) 33: 311-317 [PMID:1967314] |
| ChEMBL | In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390 | B | 6.42 | pIC50 | 384 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 539-544 |
| ChEMBL | Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand. | F | 6.42 | pIC50 | 384 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 189-192 |
| ChEMBL | Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand | B | 6.42 | pIC50 | 384 | nM | IC50 | J Med Chem (1991) 34: 2736-2746 [PMID:1680195] |
| ChEMBL | In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1 | B | 6.62 | pIC50 | 238 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 639-644 |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as low affinity state | B | 6.9 | pKd | 127 | nM | Kd | J Med Chem (1989) 32: 1198-1201 [PMID:2524592] |
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D2A expressed in COS7 cells | B | 7.62 | pKd | 24 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as high affinity state | B | 9.18 | pKd | 0.66 | nM | Kd | J Med Chem (1989) 32: 1198-1201 [PMID:2524592] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | B | 6.61 | pKi | 244 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
| ChEMBL | Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand | B | 6.66 | pKi | >217 | nM | Ki | J Med Chem (1994) 37: 2735-2753 [PMID:8064801] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in HEK293 cells | B | 7.01 | pKi | 98 | nM | Ki | Bioorg Med Chem (2008) 16: 6675-6681 [PMID:18562201] |
| ChEMBL | Displacement of [125I]iodosulpride from human D2 receptor expressed in CHO cells incubated for 40 mins by radio ligand binding assay | B | 7.09 | pKi | 82 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine D2L receptor expressed in HEK293 cells by scintillation counting analysis | B | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Displacement of [3H]raclopride from human D2L receptor expressed in HEK293 cells | B | 7.3 | pKi | 50 | nM | Ki | Eur J Med Chem (2012) 55: 255-261 [PMID:22846798] |
| ChEMBL | Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | B | 7.38 | pKi | 42 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
| ChEMBL | Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | B | 7.38 | pKi | 42 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
| ChEMBL | In vitro affinity at human cloned Dopamine receptor D2A by [3H]-raclopride displacement. | B | 7.38 | pKi | 41.9 | nM | Ki | J Med Chem (1996) 39: 3491-3502 [PMID:8784447] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells | B | 7.38 | pKi | 41.9 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| ChEMBL | Displacement of [3H]raclopride from human Dopamine receptor D2A | B | 7.38 | pKi | 41.9 | nM | Ki | J Med Chem (1996) 39: 3503-3513 [PMID:8784448] |
| ChEMBL | Ability to displace [3H]raclopride binding to cloned human Dopamine receptor D2A | B | 7.38 | pKi | 41.9 | nM | Ki | J Med Chem (1995) 38: 647-658 [PMID:7861413] |
| ChEMBL | In vitro binding affinity towards cloned human Dopamine receptor D2A using [3H]- Raclopride as radioligand. | B | 7.38 | pKi | 41.6 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 367-370 [PMID:11212112] |
| ChEMBL | Binding affinity was measured on cloned Human D2A Receptor which is labeled by [3H]raclopride | B | 7.38 | pKi | 41.6 | nM | Ki | J Med Chem (2000) 43: 1339-1349 [PMID:10753471] |
| ChEMBL | Displacement of [3H]raclopride from human cloned dopamine D2 receptor expressed in CHO cell membrane | B | 7.49 | pKi | 32 | nM | Ki | Bioorg Med Chem (2008) 16: 4563-4568 [PMID:18313931] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621]; Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163] |
| ChEMBL | Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
| ChEMBL | Compound was evaluated for the binding affinity against [3H]U-86,170-labeled D2 sites in cloned CHO cells | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (1993) 36: 1069-1083 [PMID:8097538] |
| ChEMBL | Compound was evaluated for the binding affinity against [3H]U-86,170-labeled D2 sites in cloned CHO cells | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
| ChEMBL | Displacement of [125I]7-OH-PIPAT from human D2L receptor expressed in HEK293 cell membrane | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells | B | 9.21 | pKi | 0.62 | nM | Ki | J Med Chem (2010) 53: 2510-2520 [PMID:20155917] |
| ChEMBL | Displacement of [3H]spiperone from human recombinant dopamine D2L receptor expressed in CHOFlpIn cells after 3 hrs by liquid scintillation counting | B | 6.93 | pIC50 | 117 | nM | IC50 | Medchemcomm (2013) 4: 1290-1296 |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method | F | 8.38 | pIC50 | 4.2 | nM | IC50 | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay | B | 6.24 | pEC50 | 575.44 | nM | EC50 | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
| ChEMBL | Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986] |
| ChEMBL | Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay | F | 7.9 | pEC50 | 12.7 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8 | pEC50 | 10.1 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8 | pEC50 | 10 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay | B | 8.24 | pEC50 | 5.8 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.24 | pEC50 | 5.8 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem (2008) 16: 3438-3444 [PMID:18313303] |
| ChEMBL | Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay | B | 8.77 | pEC50 | 1.7 | nM | EC50 | Medchemcomm (2013) 4: 1290-1296 |
| ChEMBL | Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.79 | pEC50 | 1.61 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 8.8 | pEC50 | 1.58 | nM | EC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Compound was tested for inhibition of [3H]spiroperidol binding against Dopamine receptor D2 | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1986) 29: 1904-1912 [PMID:3761310] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 5.8 | pKd | 1600 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 5.92 | pKd | 1200 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | B | 6.22 | pKd | 600 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | B | 6.7 | pKd | 200 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D2 receptor low binding site in Sprague-Dawley rat striatum by scintillation counting | B | 7.01 | pKi | 98 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand. | B | 7.26 | pKi | 54.95 | nM | Ki | J Med Chem (2000) 43: 599-608 [PMID:10691686] |
| ChEMBL | Ability to displace [3H]raclopride from dopamine receptor D2 in rat striatal homogenates. | B | 7.34 | pKi | 46 | nM | Ki | J Med Chem (1992) 35: 1076-1092 [PMID:1348089] |
| ChEMBL | Displacement of [3H]raclopride from rat dopamine D2(short) receptor expressed in CHOK1 cells | B | 7.49 | pKi | 32 | nM | Ki | Bioorg Med Chem (2008) 16: 4563-4568 [PMID:18313931] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand | B | 7.76 | pKi | 17.3 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
| ChEMBL | Displacement of [3H]raclopride from rat dopamine D2 receptor | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2007) 50: 171-181 [PMID:17228858] |
| ChEMBL | Displacement of [3H]raclopride from rat D2 dopamine receptor expressed in CHOK1 cells after 90 mins by liquid scintillation counter scintillation counter | B | 7.94 | pKi | 11.5 | nM | Ki | Eur J Med Chem (2011) 46: 2992-2999 [PMID:21550699] |
| ChEMBL | Displacement of [3H]raclopride from rat dopamine D2short receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 7.94 | pKi | 11.5 | nM | Ki | Bioorg Med Chem (2009) 17: 4756-4762 [PMID:19454369] |
| ChEMBL | Binding affinity at rat striatal Dopamine receptor D2 using [3H]- piperone radioligand | B | 7.95 | pKi | 11.1 | nM | Ki | J Med Chem (1990) 33: 1800-1805 [PMID:1971309] |
| ChEMBL | Displacement of [3H]raclopride from dopamine D2 receptor in rat striatal membrane | B | 7.95 | pKi | 11.1 | nM | Ki | Bioorg Med Chem (2008) 16: 4563-4568 [PMID:18313931] |
| ChEMBL | Tested for binding affinity towards rat striatal D2 receptor using [3H]NPA as radioligand | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
| ChEMBL | Displacement of [3H]neomonapride from dopamine D2 receptor in rat striatum | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2008) 51: 983-987 [PMID:18251489] |
| ChEMBL | Displacement of [3H]domperidone from dopamine D2 receptor high binding site in Sprague-Dawley rat striatum by scintillation counting | B | 8.74 | pKi | 1.8 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2 | B | 6.52 | pIC50 | 302 | nM | IC50 | J Med Chem (1991) 34: 194-197 [PMID:1671414] |
| ChEMBL | Inhibition of binding of [3H]spiroperidol to Dopamine receptor D2 in rat striatal membranes | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 883-886 [PMID:11294383] |
| 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 | 6.87 | pIC50 | 135 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| 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 | 6.93 | pIC50 | 118 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Compound was evaluated for the inhibition of [3H]spiperone binding to Dopamine receptor D2 of rat striatal membranes | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (1990) 33: 2408-2412 [PMID:1975274] |
| ChEMBL | Binding affinity against Dopamine receptor D2 from rat brain corpus striatum membrane | B | 7.18 | pIC50 | 66.7 | nM | IC50 | J Med Chem (1990) 33: 3122-3124 [PMID:2147956] |
| ChEMBL | Inhibition of [3H]haloperidol binding for Dopamine receptor D2 in rat striatal membranes. | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1990) 33: 311-317 [PMID:1967314] |
| ChEMBL | Concentration inhibiting specific binding of [3H]haloperidol to Dopamine receptor D2 from rat striatal brain. | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1990) 33: 445-450 [PMID:1967318] |
| ChEMBL | In vitro binding affinity to Dopamine receptor D2 in rat striatal membranes using D2 antagonist [3H]spiperone | B | 7.62 | pIC50 | 24.1 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 539-544 |
| ChEMBL | Affinity of the Compound for Dopamine receptor D2 in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]-spiperone as ligand; Value ranges from (20-29) | F | 7.62 | pIC50 | 24.1 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 189-192 |
| ChEMBL | Displacement of [3H]spiperone from rat striatal Dopamine receptor D2 | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 639-644 |
| ChEMBL | Compound was tested in vitro for binding affinity towards Dopamine receptor D2 in rat striatal membrane by using [3H]spiperone as radioligand | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (1991) 34: 2736-2746 [PMID:1680195] |
| ChEMBL | In vitro binding affinity towards rat Dopamine receptor D2 by [3H]spiperone displacement. | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (1990) 33: 600-607 [PMID:2405158] |
| ChEMBL | Inhibitory concentration against radioligand [3H](-)-sulpiride binding to Dopamine receptor D2 in rat | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (1999) 42: 1076-1087 [PMID:10090790] |
| ChEMBL | Inhibition of [3H]N-propylnorapomorphine as radioligand for Dopamine receptor D2 in rat striatal membranes | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (1990) 33: 311-317 [PMID:1967314] |
| ChEMBL | Affinity for [3H]N-propylnorapomorphine (NPA) Dopamine receptor D2 | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (1990) 33: 445-450 [PMID:1967318] |
| ChEMBL | In vitro agonist binding affinity was determined by displacing the [3H]N-propylnorapomorphine ([3H]NPA) in rat striatal Dopamine receptor D2 | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 639-644 |
| ChEMBL | Affinity of the Compound for Dopamine receptor D2 in rat striatal membrane was determined in vitro using Dopamine agonist [3H]N-propylnorapomorphine as ligand; Value ranges from (1.4-1.9) | F | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 189-192 |
| ChEMBL | Evaluated for the affinity against Dopamine receptor D2 in rat striatal membranes | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1988) 31: 1466-1471 [PMID:2968456] |
| ChEMBL | Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting | F | 7.28 | pEC50 | 53 | nM | EC50 | Bioorg Med Chem (2009) 17: 4756-4762 [PMID:19454369] |
| ChEMBL | Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter | F | 7.52 | pEC50 | 30 | nM | EC50 | Eur J Med Chem (2011) 46: 2992-2999 [PMID:21550699] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay | B | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay | B | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Neuroreport (1995) 6: 329-332 [PMID:7756621]; Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine D3 receptor expressed in HEK293 cells by scintillation counting analysis | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Displacement of [3H]raclopride from human D3 receptor expressed in HEK293 cells | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2012) 55: 255-261 [PMID:22846798] |
| ChEMBL | Tested for binding affinity towards human D3 receptor using [3H]spiperone as radioligand | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1994) 37: 3523-3533 [PMID:7932581] |
| ChEMBL | Displacement of [3H]domperidone from human cloned dopamine D3 receptor expressed in mouse CCL1-3 cells by scintillation counting | B | 8.59 | pKi | 2.6 | nM | Ki | ACS Med Chem Lett (2011) 2: 189-194 [PMID:21666830] |
| ChEMBL | Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 8.15 | pEC50 | 7 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
| 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 | 7.53 | pIC50 | 29.4 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| 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 | 7.57 | pIC50 | 27.2 | nM | IC50 | 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 | Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane | B | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay | B | 8.37 | pEC50 | 4.3 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.37 | pEC50 | 4.3 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay | B | 8.26 | pEC50 | 5.5 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.26 | pEC50 | 5.5 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay | B | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Nature (1991) 350: 614-9 [PMID:1826762] |
| ChEMBL | Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5.62 | pIC50 | 2398.83 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987] | ||||||||
| ChEMBL | Inhibition of biotin-labelled P4 peptide binding to MDM2 (25 to 109 residues) (unknown origin) by surface plasmon resonance method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2571-2574 [PMID:28400230] |
| ChEMBL | Inhibition of biotin-labelled L-p53 binding to L-MDM2 (25 to 109 residues) (unknown origin) by FAM labeled P4 peptide based fluorescence polarization assay | B | 6.67 | pIC50 | 215 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2571-2574 [PMID:28400230] |
| ChEMBL | Inhibition of biotin-labelled D-p53 binding to D-MDM2 (25 to 109 residues) (unknown origin) by FAM labeled P4 peptide based fluorescence polarization assay | B | 6.71 | pIC50 | 195 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2571-2574 [PMID:28400230] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Ability to displace [3H]-DPAT from 5-hydroxytryptamine 1A receptor in homogenates of bovine hippocampus. | B | 6.27 | pKi | 534 | nM | Ki | J Med Chem (1992) 35: 1076-1092 [PMID:1348089] |
| ChEMBL | Binding affinity was measured on cloned Human 5-hydroxytryptamine 1A receptor which is labeled by [3H]8-OH-DPAT | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (2000) 43: 1339-1349 [PMID:10753471] |
| ChEMBL | In vitro binding affinity towards cloned human 5-hydroxytryptamine 1A receptor expressed in Chinese hamster ovary (CHO) cells using [3H]8-OH-DPAT as radioligand | B | 6.53 | pKi | 296 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 367-370 [PMID:11212112] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| GtoPdb | - | - | 6.9 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO cells incubated for 150 mins by radio ligand binding assay | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Ability to displace [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (1995) 38: 647-658 [PMID:7861413] |
| ChEMBL | In vitro displacement of [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (1996) 39: 3503-3513 [PMID:8784448] |
| ChEMBL | In vitro affinity at 5-hydroxytryptamine 1A receptor of rat hippocampus by [3H]8-OH-DPAT displacement. | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (1996) 39: 3491-3502 [PMID:8784447] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells incubated for 40 mins by radio ligand binding assay | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT | B | 6.73 | pKi | 188 | nM | Ki | J Med Chem (2000) 43: 1339-1349 [PMID:10753471] |
| ChEMBL | In vitro binding affinity towards cloned rat 5-hydroxytryptamine 7 receptor using [3H]5-HT as radioligand | B | 6.73 | pKi | 188 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 367-370 [PMID:11212112] |
| ChEMBL | Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells | B | 6.73 | pKi | 188 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes | B | 4.51 | pIC50 | >31000 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Inhibitory concentration against radioligand [3H]3-PPP binding to Sigma opioid receptor type 1 in rat brain membrane | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1999) 42: 1076-1087 [PMID:10090790] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.68 | pIC50 | 20800 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
| TRPA1 in Human [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
| GtoPdb | Calcium imaging, patch clamp | - | 5.1 | pEC50 | - | - | - | Mol Pharmacol (2013) 83: 542-51 [PMID:23220749] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
