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ChEMBL ligand: CHEMBL2047521 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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: P15382, P51787] | ||||||||
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: 562, 564] [UniProtKB: O43525, Q9NR82] | ||||||||
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: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
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]