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

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ChEMBL ligand: CHEMBL1292 (Chlofazimine, Clofazimina, Clofazimine, Clofaziminum, Colfazimine, G 30320, G-30320, Lamprene, NSC-141046)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
Created with Highcharts 10.3.3ValuesChart context menuATP-binding cassette sub-family G member 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuBile salt export pumppKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCruzipainpKd Trypanosoma cruzipKi Trypanosoma cruzipIC50 Trypanosoma cruzipEC50 Trypanosoma cruzi0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuP-glycoprotein 1pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuPlasmodium falciparumpKd Plasmodium falciparumpKi Plasmodium falciparumpIC50 Plasmodium falciparumpEC50 Plasmodium falciparum0123456Highcharts.com
  • CoV Spike glycoprotein/Spike glycoprotein in Severe acute respiratory syndrome coronavirus 2 [ChEMBL: CHEMBL4662936] [GtoPdb: 3114] [UniProtKB: P0DTC2]
Created with Highcharts 10.3.3ValuesChart context menuSpike glycoproteinpKd Severe acute respiratory syndrome coronavirus 2pKd Severe acute respiratory syndrome coronavir…pKi Severe acute respiratory syndrome coronavirus​2pIC50 Severe acute respiratory syndrome​coronavirus 2pEC50 Severe acute respiratory syndrome​coronavirus 20123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
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
CoV Spike glycoprotein/Spike glycoprotein in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662936] [GtoPdb: 3114] [UniProtKB: P0DTC2]
ChEMBL Binding affinity to SARS-CoV-2 spike protein assessed as Kd by SPR analysis B 5.42 pKd 3820 nM Kd Eur J Med Chem (2022) 234: 114209-114209 [PMID:35279610]

ChEMBL data shown on this page come from version 35:

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]