ztz240 [Ligand Id: 7668] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1454208
  • beta-secretase 1/Beta-secretase 1 in Human [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
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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
beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
ChEMBL Binding affinity to BACE1 (unknown origin) by surface plasmon resonance spectroscopic analysis B 3.94 pKd 114000 nM Kd J Med Chem (2016) 59: 3732-3749 [PMID:26978477]
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 4.18 pIC50 66000 nM IC50 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]
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 6.01 pEC50 980 nM EC50 ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334]

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]