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

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ChEMBL ligand: CHEMBL243001
  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • ghrelin receptor/Growth hormone secretagogue receptor type 1 in Human [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2C receptor/5-hydroxytryptamine receptor 2C 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]
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]
ghrelin receptor/Growth hormone secretagogue receptor type 1 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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]