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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]