senicapoc [Ligand Id: 2331] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL405821 (ICA-17043, PF-05416266, Senicapoc)
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  • KCa3.1/Intermediate conductance calcium-activated potassium channel protein 4 in Human [ChEMBL: CHEMBL4305] [GtoPdb: 384] [UniProtKB: O15554]
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  • Nav1.1/Sodium channel protein type I alpha subunit in Human [ChEMBL: CHEMBL1845] [GtoPdb: 578] [UniProtKB: P35498]
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  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
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  • Nav1.3/Sodium channel protein type III alpha subunit in Human [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
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  • Nav1.4/Sodium channel protein type IV alpha subunit in Human [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
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  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
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  • Nav1.6/Sodium channel protein type VIII alpha subunit in Human [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0]
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  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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  • Kv7.1/Voltage-gated potassium channel subunit Kv7.1 in Human [ChEMBL: CHEMBL1866] [GtoPdb: 560] [UniProtKB: P51787]
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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 channel B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
KCa3.1/Intermediate conductance calcium-activated potassium channel protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4305] [GtoPdb: 384] [UniProtKB: O15554]
ChEMBL Inhibition of gardos channel (unknown origin) B 4.96 pIC50 11000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
ChEMBL Inhibition of Gardos channel in human RBC assessed as inhibition of ionomycin-stimulated [86Rb] efflux B 7.92 pIC50 12 nM IC50 J Med Chem (2008) 51: 976-982 [PMID:18232633]
GtoPdb - - 7.96 pIC50 11 nM IC50 Blood (2003) 101: 2412-8 [PMID:12433690]
ChEMBL Inhibition of Kca 3.1 (unknown origin) B 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Protein Red in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321616] [UniProtKB: Q13123]
ChEMBL Inhibition of IK (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.1/Sodium channel protein type I alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1845] [GtoPdb: 578] [UniProtKB: P35498]
ChEMBL Inhibition of voltage-gated Na channel 1.1 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
ChEMBL Inhibition of voltage-gated Na channel 1.2 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.3/Sodium channel protein type III alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
ChEMBL Inhibition of voltage-gated Na channel 1.3 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
ChEMBL Inhibition of voltage-gated Na channel 1.4 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Inhibition of voltage-gated Na channel 1.7 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Nav1.6/Sodium channel protein type VIII alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0]
ChEMBL Inhibition of voltage-gated Na channel 1.6 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
ChEMBL Inhibition of voltage-gated K channel 1.5 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
Kv7.1/Voltage-gated potassium channel subunit Kv7.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1866] [GtoPdb: 560] [UniProtKB: P51787]
ChEMBL Inhibition of voltage-gated K channel 7.1 (unknown origin) B 6 pIC50 >1000 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]

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]