ICA-069673 [Ligand Id: 14111] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2047521
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
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  • Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human [ChEMBL: CHEMBL2221348] [GtoPdb: 562561] [UniProtKB: O43525O43526]
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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 B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of NaV1.5 B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
ChEMBL Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting F 4 pIC50 >100000 nM IC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]
Kv7.3/Kv7.5/Voltage-gated potassium channel KCNQ3/KCNQ5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883311] [GtoPdb: 562564] [UniProtKB: O43525Q9NR82]
ChEMBL Agonist activity at KCNQ3/KCNQ5 expressed in CHO cells increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting F 4.84 pEC50 14300 nM EC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]
Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221348] [GtoPdb: 562561] [UniProtKB: O43525O43526]
GtoPdb Assessed as activation of KCNQ2/KCNQ3 channels expressed in CHO. - 6.16 pEC50 690 nM EC50 ACS Med Chem Lett (2011) 2: 481-4 [PMID:24900334]
ChEMBL Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting F 6.16 pEC50 690 nM EC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]

ChEMBL data shown on this page come from version 35:

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]