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 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]