YIL781 [Ligand Id: 3538] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL243001
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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
ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
GtoPdb - - 7.77 pKi 17 nM Ki Endocrinology (2007) 148: 5175-85 [PMID:17656463]
ChEMBL Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting B 8.4 pKi 4 nM Ki Bioorg Med Chem Lett (2012) 22: 2271-2278 [PMID:22342626]
Ghrelin receptor in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5015] [UniProtKB: Q8MHZ5]
ChEMBL Displacement of [125I]ghrelin from ovine recombinant GHSR1a expressed in HEK293F cells after 6 hrs by scintillation proximity assay B 7.77 pKi 17 nM Ki J Med Chem (2007) 50: 5202-5216 [PMID:17887659]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Erg by patch clamp assay B 5.79 pIC50 1621.81 nM IC50 Bioorg Med Chem Lett (2012) 22: 2271-2278 [PMID:22342626]
ChEMBL Inhibition of human Erg by patch clamp assay B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem Lett (2012) 22: 2271-2278 [PMID:22342626]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [125I]DIO from 5HT2c receptor B 6 pKi >1000 nM Ki J Med Chem (2007) 50: 5202-5216 [PMID:17887659]

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]