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

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ChEMBL ligand: CHEMBL1043 (Diaphenylsulfone, Diaminodiphenylsulfone, Dapsone, NSC-6091D, NSC-6091, Aczone, J04BA02)
  • 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]
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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]