NS11757 [Ligand Id: 2944] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL511710 (NS-11757)
  • KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Human [ChEMBL: CHEMBL2369] [GtoPdb: 381] [UniProtKB: Q92952]
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  • KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Human [ChEMBL: CHEMBL4469] [GtoPdb: 382] [UniProtKB: Q9H2S1]
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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2369] [GtoPdb: 381] [UniProtKB: Q92952]
ChEMBL Inhibition of human SK1 channel by inside-out patch clamp technique B 7.27 pKd 54 nM Kd J Med Chem (2008) 51: 7625-7634 [PMID:18998663]
KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4469] [GtoPdb: 382] [UniProtKB: Q9H2S1]
ChEMBL Inhibition of human SK2 channel by inside-out patch clamp technique B 7.33 pKd 47 nM Kd J Med Chem (2008) 51: 7625-7634 [PMID:18998663]
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 human SK3 channel by inside-out patch clamp technique B 7.22 pKd 60 nM Kd J Med Chem (2008) 51: 7625-7634 [PMID:18998663]
ChEMBL Inhibition of human SK3 channel expressed in HEK293 cells assessed as Ca2+ induced current after drug wash out by whole cell patch clamp technique in presence of bicuculline methobromide B 8.11 pKd 7.8 nM Kd 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 5.74 pEC50 1810 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 8.04 pKd 9.1 nM Kd J Med Chem (2008) 51: 7625-7634 [PMID:18998663]
GtoPdb - - 8.1 pKd - - - J Med Chem (2008) 51: 7625-34 [PMID:18998663]

ChEMBL data shown on this page come from version 32:

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]