indapamide [Ligand Id: 7203] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL406 (Arifon, Bajaten, Cardide sr, Damide, Ethibide xl, Flubest, Fludex, Fludin, Flupamid, Indaflex, Indamide, Indamol, Indapamide, Indaxa 2.5, Indipam xl, Ipamix, KYD-041, Lorvas, Lozol, Mapemid xl, Natrilix, Natrilix sr, Natrix, Nindaxa 2.5, Noranat, NSC-757075, Opumide 2.5, Rawel xl, S-1520, SE-1520, Tandix, Tensaid xl, Tertensif, Varbim xl, Veroxil)
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
  • carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1]
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.53 pIC50 2918 nM IC50 DrugMatrix in vitro pharmacology data
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 1 by thermal shift assay B 5 pKd 10000 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) by thermal shift assay B 5 pKd 10000 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
ChEMBL Inhibition of human recombinant full length CA1 by stopped-flow CO2 hydration method B 4.28 pKi 51900 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 2 by thermal shift assay B 6.52 pKd 300 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 2 by thermal shift assay B 6.52 pKd 300 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 2 by isothermal titration calorimetry assay B 6.7 pKd 200 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Inhibition of human recombinant full length CA2 by stopped-flow CO2 hydration method B 5.6 pKi 2520 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
ChEMBL Inhibition of human recombinant full length CA4 by stopped-flow CO2 hydration method B 6.67 pKi 213 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method B 7.44 pKi 36 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
ChEMBL Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5A expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay B 6.17 pKd 670 nM Kd Bioorg Med Chem (2018) 26: 675-687 [PMID:29305297]
ChEMBL Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5A expressed in Escherichia coli BL21 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay B 8.16 pKd 6.96 nM Kd Bioorg Med Chem (2018) 26: 675-687 [PMID:29305297]
ChEMBL Inhibition of human recombinant full length CA5A by stopped-flow CO2 hydration method B 6.05 pKi 890 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
ChEMBL Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5B (40 to 317 residues) expressed in Escherichia coli Rosetta 2 (DE3) in presence of ANS by fluorescent thermal shift assay B 7.23 pKd 59 nM Kd Bioorg Med Chem (2018) 26: 675-687 [PMID:29305297]
ChEMBL Binding affinity to recombinant human full length N-terminal His6-tagged mitochondrial carbonic anhydrase 5B (40 to 317 residues) expressed in Escherichia coli Rosetta 2 (DE3) assessed as intrinsic dissociation constant in presence of ANS by fluorescent thermal shift assay B 9.34 pKd 0.46 nM Kd Bioorg Med Chem (2018) 26: 675-687 [PMID:29305297]
ChEMBL Inhibition of human recombinant full length CA5B by stopped-flow CO2 hydration method B 6.56 pKi 274 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 6 expressed in Escherichia coli Rosetta2 (DE3) by thermal shift assay B 6.6 pKd 250 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
ChEMBL Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method B 5.79 pKi 1606 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 7 by isothermal titration calorimetry assay B 5.74 pKd 1800 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 7 by thermal shift assay B 6.52 pKd 300 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 7 by thermal shift assay B 6.52 pKd 300 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
ChEMBL Inhibition of human recombinant full length CA7 by stopped-flow CO2 hydration method B 9.64 pKi 0.23 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
ChEMBL Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay B 9.64 pKi 0.23 nM Ki Eur J Med Chem (2014) 71: 105-111 [PMID:24287559]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 12 by thermal shift assay B 5.85 pKd 1400 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
ChEMBL Inhibition of human recombinant CA12 catalytic domain by stopped-flow CO2 hydration method B 8 pKi 10 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 13 by isothermal titration calorimetry assay B 6.7 pKd 200 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 13 by thermal shift assay B 7 pKd 100 nM Kd Bioorg Med Chem (2010) 18: 7357-7364 [PMID:20926301]
ChEMBL Binding affinity to human recombinant carbonic anhydrase 13 by thermal shift assay B 7 pKd 100 nM Kd Bioorg Med Chem (2013) 21: 6937-6947 [PMID:24103428]
carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1]
ChEMBL Inhibition of mouse recombinant full length CA13 by stopped-flow CO2 hydration method B 7.89 pKi 13 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]
carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
ChEMBL Inhibition of human recombinant full length CA14 by stopped-flow CO2 hydration method B 5.31 pKi 4950 nM Ki Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014]

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]