TRAM-34 [Ligand Id: 2336] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL498270
  • KCa3.1/Intermediate conductance calcium-activated potassium channel protein 4 in Human [ChEMBL: CHEMBL4305] [GtoPdb: 384] [UniProtKB: O15554]
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  • Kv1.3/Voltage-gated potassium channel subunit Kv1.3 in Human [ChEMBL: CHEMBL4633] [GtoPdb: 540] [UniProtKB: P22001]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KCa3.1/Intermediate conductance calcium-activated potassium channel protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4305] [GtoPdb: 384] [UniProtKB: O15554]
GtoPdb - - 8 pKd - - - Proc Natl Acad Sci USA (2000) 97: 8151-6 [PMID:10884437];
Circulation (2003) 108: 1119-25 [PMID:12939222]
ChEMBL Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2009) 19: 2299-2304 [PMID:19282171]
ChEMBL Inhibition of IK1 B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2009) 19: 2299-2304 [PMID:19282171]
Kv1.3/Voltage-gated potassium channel subunit Kv1.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4633] [GtoPdb: 540] [UniProtKB: P22001]
ChEMBL Inhibition of cloned Kv1.3 channel expressed in mammalian cells by whole cell patch clamp assay B 5.3 pIC50 5000 nM IC50 Bioorg Med Chem Lett (2009) 19: 2299-2304 [PMID:19282171]

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]