clofazimine [Ligand Id: 9184] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1292 (Clofazimine, NSC-141046, Lamprene, G 30320, G-30320)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) F 4.54 pIC50 28700 nM IC50 Pharm. Res. (2003) 20: 537-544 [PMID:12739759]
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 B 4.4 pIC50 40000 nM IC50 J. Med. Chem. (2010) 53: 4259-4265 [PMID:20426472]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine in presence of 0.01% Triton B 4.4 pIC50 40000 nM IC50 Eur. J. Med. Chem. (2015) 93: 338-348 [PMID:25707014]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (2010) 53: 4259-4265 [PMID:20426472]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine in absence of 0.01% Triton B 5.22 pIC50 6000 nM IC50 Eur. J. Med. Chem. (2015) 93: 338-348 [PMID:25707014]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.96 pIC50 1100 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 6 pIC50 1000 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 6.22 pIC50 600 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay F 5.15 pIC50 7020 nM IC50 Bioorg. Med. Chem. (2015) 23: 55-65 [PMID:25497962]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay F 5.32 pIC50 4820 nM IC50 Bioorg. Med. Chem. (2015) 23: 55-65 [PMID:25497962]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.39 pIC50 4100 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning

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]