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) |
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| 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]
