(+)-butaclamol [Ligand Id: 62] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8514 (Butaclamol)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • 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]
  • 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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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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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]
GtoPdb - - 8.5 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762];
J Biol Chem (1994) 269: 27925-31 [PMID:7525564]
ChEMBL Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. (2016) 24: 2060-2071 [PMID:27032890]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Affinity towards dopamine receptor D1 in rat corpus striatum tissue. B 9 pKi 9 - -Log K0.5 J. Med. Chem. (1999) 42: 3217-3226 [PMID:10464009]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 8.7 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989];
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010];
J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]
ChEMBL Displacement of [3H]methyl-spiperone from human recombinant D2S receptor in HEK293 cells after 60 mins by scintillation counting B 9.57 pKi 0.27 nM Ki J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Displacement of [3H]methylspiperone from human recombinant D2S receptor expressed in HEK293 cells B 10.4 pKi 0.04 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]methylspiperone from human D2S receptor expressed in HEK293 cells B 10.4 pKi 0.04 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Antagonist activity at human recombinant at D2S receptor assessed as inhibition of dopamine-induced cAMP accumulation F 8.3 pIC50 5 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]methylspiperone from human recombinant Dopamine D2S receptor expressed in HEK293 cells B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]methyl-spiperone from human recombinant D2S receptor in HEK293 cells after 60 mins by scintillation counting B 9.09 pIC50 0.81 nM IC50 J Med Chem (2017) 60: 349-361 [PMID:27997171]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Inhibition of binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membranes B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (1994) 37: 99-104 [PMID:8289207]
ChEMBL In vitro binding affinity measured on dopamine receptor D2 using [3H]spiroperidol as radioligand. B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (1995) 38: 942-949 [PMID:7699710]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 8 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
J Pharmacol Exp Ther (1995) 275: 1355-66 [PMID:8531103];
J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]
ChEMBL Displacement of [3H]methylspiperone from human recombinant D3 receptor expressed in CHO cells B 10.4 pKi 0.04 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]methylspiperone from human dopamine D3 receptor expressed in CHO cells B 10.4 pKi 0.04 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Antagonist activity at human recombinant at D3 receptor assessed as inhibition of dopamine-induced cAMP accumulation F 7.8 pIC50 16 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Antagonist activity against human recombinant dopmaine D3 receptor expressed in CHOK1 cells assessed as reduction in dopamine-induced cAMP levels B 7.8 pIC50 16 nM IC50 Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]methylspiperone from human recombinant Dopamine D3 receptor expressed in CHO cells B 8.8 pIC50 1.6 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7.5 pKi - - - Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 8.41 pKi 3.91 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 7.5 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]
GtoPdb - - 7 pKi - - - Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
ChEMBL Binding affinity towards 5-hydroxytryptamine 7 receptor B 7.2 pKi 63.1 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1097-1100 [PMID:10843226]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 6.4 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.6 pKi - - - Mol Pharmacol (1990) 38: 604-9 [PMID:2233697]
D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 6.3 pKi - - - Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 7.6 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]