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 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]