gepirone [Ligand Id: 12930] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL284092 (Ariza, BMY-13805, Gepirona, Gepirone, ORG-13011, Variza) |
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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 | Displacement of [3H]methylspiperone from human D2 receptor expressed in HEK cells | B | 5.36 | pKi | 4320 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Binding affinity to D2 receptor by radioligand binding assay | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 7.1 | pKd | 79.43 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Binding affinity to 5-HT1A (unknown origin) | B | 7.5 | pKi | 31.8 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor in HEK293 cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in human CYP3A4 assay | B | 6.94 | pIC50 | 114 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1709-1712 [PMID:15026055] |
| ChEMBL | Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay | F | 6.54 | pEC50 | 288 | nM | EC50 | J Med Chem (2006) 49: 3116-3135 [PMID:16722631] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (1988) 31: 1968-1971 [PMID:3172131] |
| ChEMBL | In vitro ability to displace [3H]8-hydroxy-2-(di-n-propylamino) tetralin binding from 5-hydroxytryptamine 1A receptor site in rat brain hippocampus | B | 7.5 | pKi | 31.8 | nM | Ki | J Med Chem (1992) 35: 2369-2374 [PMID:1535661] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to 5-HT2A (unknown origin) | B | 5.44 | pKi | 3630 | nM | Ki | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
ChEMBL data shown on this page come from version 34:
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]
