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 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]