WAY-181187 [Ligand Id: 3240] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL392760 (WAY-181187)
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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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-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Inhibition of human 5HT2B receptor expressed in CHO cells B 6.34 pKi 458 nM Ki J. Med. Chem. (2007) 50: 5535-5538 [PMID:17948978]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibition of human 5HT2C receptor expressed in CHO cells B 6.91 pKi 124 nM Ki J. Med. Chem. (2007) 50: 5535-5538 [PMID:17948978]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells B 8.7 pKi 2 nM Ki J. Med. Chem. (2007) 50: 5535-5538 [PMID:17948978]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting B 8.7 pKi 2 nM Ki J. Med. Chem. (2009) 52: 675-687 [PMID:19159187]
ChEMBL Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells B 8.7 pKi 2 nM Ki J. Med. Chem. (2009) 52: 6153-6157 [PMID:19739674]
ChEMBL Binding affinity to 5HT6 receptor B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. (2009) 17: 7387-7397 [PMID:19758807]
ChEMBL Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter B 8.7 pKi 2 nM Ki J. Med. Chem. (2015) 58: 7901-7912 [PMID:26099069]
GtoPdb - - 8.7 pKi - - - Neuropsychopharmacology (2008) 33: 1323-35 [PMID:17625499]
ChEMBL Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production F 8.19 pEC50 6.5 nM EC50 J. Med. Chem. (2007) 50: 5535-5538 [PMID:17948978]
ChEMBL Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay F 8.19 pEC50 6.5 nM EC50 J. Med. Chem. (2009) 52: 6153-6157 [PMID:19739674]
ChEMBL Agonist activity at 5HT6 receptor F 8.19 pEC50 6.5 nM EC50 Bioorg. Med. Chem. (2009) 17: 7387-7397 [PMID:19758807]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 6.17 pKi 679 nM Ki J. Med. Chem. (2007) 50: 5535-5538 [PMID:17948978]

ChEMBL data shown on this page come from version 31:

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]