CGS-12066 [Ligand Id: 109] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL27403 (CGS-12066B)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
  • Serotonin 1d (5-HT1d) receptor in Pig [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
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  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]