(+)-butaclamol [Ligand Id: 62] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8514 (Butaclamol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method | B | 8.37 | pKi | 4.3 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) | B | 8.39 | pKi | 4.04 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127305-127305 [PMID:32631525] |
| 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] |
| ChEMBL | Displacement of [3H]SCH-23390 from human dopamine D1 receptor assessed as inhibition constant | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| ChEMBL | Binding affinity to human D1 receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| D1 receptor/D(1A) dopamine 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/D(2) dopamine 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 | Binding affinity to D2S (unknown origin) assessed as inhibition constant | B | 9.04 | pKi | 0.91 | nM | Ki | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| 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 | Inhibition of D2S (unknown origin) | B | 8.57 | pIC50 | 2.7 | nM | IC50 | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| 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] |
| D3 receptor/D(3) dopamine 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 dopamine D3 receptor expressed in HEK-T cells assessed as inhibition of dopamine-induced cAMP production preincubated for 5 followed by dopamine and NKH-477 addition and measured after 30 mins by fluorescence based analysis | F | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| 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 in Rat [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - | Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010] |
| 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] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
| 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| 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 36:
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]
