NS8593 [Ligand Id: 2318] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL510780 (NS-8593)
  • KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6]
  • KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605]
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  • KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
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  • KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
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  • TRPM7 in Mouse [GtoPdb: 499] [UniProtKB: Q923J1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6]
ChEMBL Inhibition of wild type human SK3 channel expressed in HEK293 cells B 7 pKd 100 nM Kd J. Med. Chem. (2008) 51: 7625-7634 [PMID:18998663]
GtoPdb - - 6.1 pIC50 - - - Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279]
ChEMBL Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique in presence of 500 nM Ca2+ B 5.66 pEC50 2200 nM EC50 J. Med. Chem. (2008) 51: 7625-7634 [PMID:18998663]
ChEMBL Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique B 6.4 pEC50 400 nM EC50 J. Med. Chem. (2008) 51: 7625-7634 [PMID:18998663]
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605]
ChEMBL Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique B 7.11 pKd 77 nM Kd J. Med. Chem. (2008) 51: 7625-7634 [PMID:18998663]
ChEMBL Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells B 4.3 pKi >50000 nM Ki J. Med. Chem. (2008) 51: 7625-7634 [PMID:18998663]
KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
GtoPdb - - 6.4 pIC50 400 nM IC50 Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279]
KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
GtoPdb - - 6.2 pIC50 - - - Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279]
TRPM7 in Mouse [GtoPdb: 499] [UniProtKB: Q923J1]
GtoPdb - - 5.8 pIC50 1600 nM IC50 Br J Pharmacol (2012) 166: 1357-76 [PMID:22242975]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]