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]
ChEMBL Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method B 8.32 pKi 4.8 nM Ki Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
ChEMBL Displacement of [3H]-LSD from human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition constant incubated for 120 mins by Topcount scintillation counting analysis B 8.32 pKi 4.8 nM Ki J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
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 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]