YM348 [Ligand Id: 230] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL407909 (YM-348)
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]5-HT from human 5HT2A receptor expressed in CHO cells B 7.89 pKi 13 nM Ki Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Displacement of [3H]5-HT from human 5HT2A receptor expressed in CHO cells B 7.89 pKi 13 nM Ki Bioorg Med Chem (2008) 16: 3309-3320 [PMID:18083579]
ChEMBL Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis F 7.03 pEC50 93 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Agonist activity at Homo sapiens (human) 5-HT2A receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay B 7.03 pEC50 93 nM EC50 Med Chem Res (2012) 21: 1491-1508
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells B 8.6 pKi 2.5 nM Ki Bioorg Med Chem (2008) 16: 3309-3320 [PMID:18083579]
ChEMBL Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis F 8.49 pEC50 3.2 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 9 pKi - - - Eur J Pharmacol (2004) 483: 37-43 [PMID:14709324]
ChEMBL Displacement of [3H]5-HT from human 5HT2C receptor expressed in CHO cells B 9.05 pKi 0.89 nM Ki Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Displacement of [3H]5-HT from human 5HT2C receptor expressed in CHO cells B 9.05 pKi 0.89 nM Ki Bioorg Med Chem (2008) 16: 3309-3320 [PMID:18083579]
ChEMBL Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis F 9 pEC50 1 nM EC50 Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544]
ChEMBL Agonist activity at Homo sapiens (human) 5-HT2C receptor assessed as 5-HT-induced phosphoinositide hydrolysis by cell based assay B 9 pEC50 1 nM EC50 Med Chem Res (2012) 21: 1491-1508

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]