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]
  • This target only has 1 pki data point
1 CHEMBL27403_lig_chart_1 Serotonin 1a (5-HT1a) receptor HumanRat
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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]
  • This target only has 1 pki data point
2 CHEMBL27403_lig_chart_2 5-HT1B receptor HumanRat
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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]
  • This target only has 1 pki data point
3 CHEMBL27403_lig_chart_3 Serotonin 1d (5-HT1d) receptor HumanPig
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  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
  • This target only has 0 pki data point
4 CHEMBL27403_lig_chart_4 Serotonin 2a (5-HT2a) receptor Bovine
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
5 CHEMBL27403_lig_chart_5 Serotonin 2c (5-HT2c) receptor Human
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6 CHEMBL27403_lig_chart_6 Serotonin 3 (5-HT3) receptor HumanRat
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
7 CHEMBL27403_lig_chart_7 5-HT2A receptor Human
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
8 CHEMBL27403_lig_chart_8 5-HT2B receptor Human
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  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • This target only has 1 pki data point
9 CHEMBL27403_lig_chart_9 5-HT6 receptor Rat
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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. U.S.A. (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. U.S.A. (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: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
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: 373374] [UniProtKB: P35563Q9JJ16]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]