[3H]N-methylspiperone [Ligand Id: 196] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267932 (3-n-methylspiperone, N-methylspiroperidol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Affinity constant of compound was evaluated in human brain | B | 10.01 | pKd | 0.1 | nM | Kd | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 9.88 | pKi | 0.13 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Evaluated in vivo for the affinity towards Dopamine receptor D2 of rat striatal tissue | B | 10.01 | pKd | 0.1 | nM | Kd | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
| ChEMBL | Binding affinity towards Dopamine receptor D2 by displacing [3H]spiperone | B | 9.93 | pKi | 0.12 | nM | Ki | J Med Chem (1992) 35: 423-430 [PMID:1531364] |
| GtoPdb | - | - | 10.7 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 9.58 | pKi | 0.27 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| 5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 9.1 | pKd | - | - | - | Mol Pharmacol (2000) 58: 877-86 [PMID:11040033] |
| D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
