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ChEMBL ligand: CHEMBL27403 (CGS-12066B) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor | B | 7.33 | pIC50 | 46.77 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor was measured using [3H]8-OH-DPAT as radioligand | B | 7.33 | pIC50 | 46.77 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 8.02 | pKi | 9.55 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
ChEMBL | Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
GtoPdb | - | - | 8.7 | pKi | - | - | - |
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; Eur J Pharmacol (1999) 380: 171-81 [PMID:10513577] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | Binding affinity for 5-hydroxytryptamine 1B receptor | B | 6.47 | pIC50 | 338.84 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand | B | 6.47 | pIC50 | 338.84 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
GtoPdb | - | - | 8.6 | pKi | - | - | - |
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; Mol Pharmacol (1991) 40: 143-8 [PMID:1652050] |
ChEMBL | Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400] | ||||||||
ChEMBL | Binding affinity for 5-hydroxytryptamine 1D receptor | B | 6.91 | pIC50 | 123.03 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor was measured using [3H]5-HT as radioligand | B | 6.91 | pIC50 | 123.03 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor | B | 4.73 | pIC50 | 18620.87 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligand | B | 4.73 | pIC50 | 18620.87 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
GtoPdb | - | - | 5.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 2C receptor | B | 4.01 | pIC50 | 97723.72 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
ChEMBL | Binding affinity against 5-Hydroxytryptamine 2C Receptor was measured using [3H]N-methyl-mesulergine as radioligand | B | 4.01 | pIC50 | 97723.72 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
ChEMBL | Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
ChEMBL | Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | B | 5.88 | pIC50 | 1318.26 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 3 receptor | B | 5.88 | pIC50 | 1318.26 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
GtoPdb | - | - | 5.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 6.1 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 6.1 | pKi | - | - | - | Mol Pharmacol (1993) 43: 320-7 [PMID:7680751] |
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]