WAY-208466 [Ligand Id: 8429] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL571858 (WAY-208466)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2 receptor expressed in CHO-K1 cells B 5.3 pIC50 <5000 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO-K1 cells B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO-K1 cells B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [125I]DOI from human cloned 5HT2A receptor expressed in CHO cells B 6.45 pIC50 351 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]5-HT from human cloned 5HT2C receptor expressed in CHO cells B 6.19 pIC50 644 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
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 HT6 receptor expressed in human HeLa cells B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 6935-6938 [PMID:19884004]
ChEMBL Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells B 8.32 pKi 4.8 nM Ki Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
ChEMBL Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter B 8.32 pKi 4.8 nM Ki J. Med. Chem. (2015) 58: 7901-7912 [PMID:26099069]
GtoPdb - - 8.32 pKi 4.8 nM Ki Bioorg Med Chem (2009) 17: 5153-63 [PMID:19523834]
ChEMBL Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay F 8.14 pEC50 7.3 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 6935-6938 [PMID:19884004]
ChEMBL Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA F 8.14 pEC50 7.3 nM EC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]
ChEMBL Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay B 8.14 pEC50 7.3 nM EC50 J. Med. Chem. (2015) 58: 7901-7912 [PMID:26099069]
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 cloned 5HT7 receptor expressed in CHO cells B 5.32 pIC50 4764 nM IC50 Bioorg. Med. Chem. (2009) 17: 5153-5163 [PMID:19523834]

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]