apomorphine [Ligand Id: 33] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL53 (Apomorphine, VR040, APL-130277, VR-040)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Mouse [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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  • TRPA1 in Human [GtoPdb: 485] [UniProtKB: O75762]
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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]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 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 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 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 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]
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 [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 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 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 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 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 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 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 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: 1053-1068 [PMID:8097537]
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 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 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
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