(+)-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/Dopamine D1 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 | 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/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 | F | 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 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]
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