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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL392760 (WAY-181187)
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
There should be some charts here, you may need to enable JavaScript!
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 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]