compound 6 [PMID: 29579323] [Ligand Id: 10039] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1408302
  • TRPM4/Transient receptor potential cation channel subfamily M member 4 in Human [ChEMBL: CHEMBL1628469] [GtoPdb: 496] [UniProtKB: Q8TD43]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPM4/Transient receptor potential cation channel subfamily M member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628469] [GtoPdb: 496] [UniProtKB: Q8TD43]
ChEMBL Inhibition of Flag-tagged TRPM4 (unknown origin) expressed in HEK293 cells assessed as reduction in intracellular Na+ influx after 45 mins by ANG2 dye-based fluorescence assay B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2019) 166: 167-177 [PMID:30708257]
GtoPdb - - 6.4 pIC50 400 nM IC50 Cancers (Basel) (2021) 13: [PMID:34771564]
GtoPdb In a fluorescence cell‐based screening assay that monitors Na+ influx using the intracellular Na+ specific dye Asante natrium green‐II. - 6.4 pIC50 400 nM IC50 Br J Pharmacol (2018) 175: 2504-2519 [PMID:29579323]

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]