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

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ChEMBL ligand: CHEMBL510780 (NS-8593)
  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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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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  • TRPM7/Transient receptor potential cation channel subfamily M member 7 in Mouse [ChEMBL: CHEMBL3714706] [GtoPdb: 499] [UniProtKB: Q923J1]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.86 pIC50 1393 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
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]
TRPM7/Transient receptor potential cation channel subfamily M member 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714706] [GtoPdb: 499] [UniProtKB: Q923J1]
ChEMBL Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in presence of 300 uM free intracellular Mg2+ by whole cell patch clamp analysis B 5.23 pIC50 5900 nM IC50 J Nat Prod (2024) 87: 783-797 [PMID:38537009]
ChEMBL Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in presence of 780 uM free intracellular Mg2+ by whole cell patch clamp analysis B 5.41 pIC50 3900 nM IC50 J Nat Prod (2024) 87: 783-797 [PMID:38537009]
ChEMBL Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in absence of intracellular Mg2+ by whole cell patch clamp analysis B 5.8 pIC50 1600 nM IC50 J Nat Prod (2024) 87: 783-797 [PMID:38537009]
GtoPdb - - 5.8 pIC50 1600 nM IC50 Br J Pharmacol (2012) 166: 1357-76 [PMID:22242975]
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]

ChEMBL data shown on this page come from version 34:

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]