SB 221284 [Ligand Id: 191] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL276140 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of heterologously expressed human Cytochrome P450 19A1 at 100 uM | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells using [3H]ketanserin as radioligand | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (1998) 41: 1598-1612 [PMID:9572885] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (1998) 41: 1598-1612 [PMID:9572885] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine as radioligand | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (1998) 41: 1598-1612 [PMID:9572885] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
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]
