dapsone [Ligand Id: 10934] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1043 (Aczone, Dapsone, Dapsonum, Diaminodiphenylsulfone, Diaphenylsulfone, J04BA02, Novophone, NSC-6091, NSC-6091D, Servidapson)
  • Dihydrofolate reductase in Pneumocystis carinii [ChEMBL: CHEMBL1926] [UniProtKB: P16184]
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  • Dihydropteroate synthetase, putative in Plasmodium berghei str. ANKA [ChEMBL: CHEMBL1741265] [UniProtKB: A0A113T0T6]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase in Plasmodium falciparum [GtoPdb: 3065]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dihydrofolate reductase in Pneumocystis carinii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926] [UniProtKB: P16184]
ChEMBL Inhibitory activity was determined against dihydrofolate reductase in Pneumocystis carinii. B 5.82 pIC50 1500 nM IC50 J Med Chem (1995) 38: 4739-4759 [PMID:7490723]
Dihydropteroate synthetase, putative in Plasmodium berghei str. ANKA (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741265] [UniProtKB: A0A113T0T6]
ChEMBL Inhibitory activity against dihydropteroic acid synthase (SYN) from Plasmodium berghei B 4.91 pIC50 12410 nM IC50 J Med Chem (2004) 47: 240-253 [PMID:14695838]
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of MPO (unknown origin) B 6.38 pIC50 420 nM IC50 Bioorg Med Chem Lett (2019) 29: 1-7 [PMID:30466896]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.74 pIC50 18000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013]
ChEMBL Antimalarial activity against Plasmodium vivax infected in human blood incubated for 24 to 36 hrs F 5.79 pIC50 1625 nM IC50 Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins F 6.74 pKi 183 nM Ki Bioorg Med Chem (2013) 21: 4614-4627 [PMID:23787290]
Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase in Plasmodium falciparum [GtoPdb: 3065]
GtoPdb Enzyme inhibition assay. - 5.22 pKi 6000 nM Ki Antimicrob Agents Chemother (1991) 35: 267-71 [PMID:2024960]

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]