GSK3527497 [Ligand Id: 12560] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4550510
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  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
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  • TRPV6 in Human [GtoPdb: 512] [UniProtKB: Q9H1D0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by electrophysiology B 4.7 pIC50 20000 nM IC50 J Med Chem (2019) 62: 9270-9280 [PMID:31532662]
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
ChEMBL Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ flux preincubated for 10 mins followed by agonist addition by Fluo-4 AM dye based FLIPR assay B 7.92 pIC50 12 nM IC50 J Med Chem (2019) 62: 9270-9280 [PMID:31532662]
TRPV6 in Human [GtoPdb: 512] [UniProtKB: Q9H1D0]
GtoPdb - - 7.92 pIC50 12 nM IC50 J Med Chem (2019) 62: 9270-9280 [PMID:31532662]

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]