epiroprim [Ligand Id: 12327] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280378 (Epiroprim, Epiroprima, Epiroprime, RO 11-8958, TCMDC-137295) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Bacterial dihydrofolate reductase in Bacteria (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364669] [UniProtKB: P0ABQ4] | ||||||||
| ChEMBL | In vitro inhibition of Pneumocystis carinii (Pc) dihydrofolate reductase. | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2002) 45: 233-241 [PMID:11754594] |
| Dihydrofolate reductase in Lactobacillus casei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2902] [UniProtKB: P00381] | ||||||||
| ChEMBL | Inhibitory activity against Lactobacillus casei dihydrofolate reductase | B | 7.33 | pKi | 46.77 | nM | Ki | J Med Chem (1989) 32: 1895-1905 [PMID:2502631] |
| Dihydrofolate reductase in Mycobacterium avium (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5457] [UniProtKB: O30463] | ||||||||
| ChEMBL | Concentration required to inhibit the Mycobacterium avium Dihydrofolate reductase by 50% was determined | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| Dihydrofolate reductase in Pneumocystis carinii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926] [UniProtKB: P16184] | ||||||||
| ChEMBL | Inhibition of dihydrofolate reductase (DHFR) from Pneumocystis carinii. | B | 7.76 | pKi | 17.38 | nM | Ki | J Med Chem (1995) 38: 967-972 [PMID:7699713] |
| ChEMBL | Binding affinity was reported with purified recombinant Pneumocystis carinii Dihydrofolate reductase | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Concentration required to inhibit the Pneumocystis carinii Dihydrofolate reductase by 50% was determined; Range: 2600-3000 | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase in Pneumocystis carinii at 37 centigrade. | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Inhibition of Dihydrofolate Reductase of Pneumocystis carinii. | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1997) 40: 479-485 [PMID:9046338] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii was evaluated using 90 uM dihydrofolic acid as substrate | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1997) 40: 3040-3048 [PMID:9301666] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from pneumocystis carinii | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibition of Pneumocystis carinii Dihydrofolate Reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 3694-3699 [PMID:9357537] |
| Dihydrofolate reductase in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2425] [UniProtKB: Q07422] | ||||||||
| ChEMBL | Concentration required to inhibit the Toxoplasma gondii Dihydrofolate reductase by 50% was determined (reported by Hoffman-LaRoche group) | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from Toxoplasma gondii | B | 6.32 | pIC50 | 480 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibition of Dihydrofolate Reductase of Toxoplasma gondii. | B | 6.32 | pIC50 | 480 | nM | IC50 | J Med Chem (1997) 40: 479-485 [PMID:9046338] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii was evaluated using 90 uM dihydrofolic acid as substrate | B | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (1997) 40: 3040-3048 [PMID:9301666] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibition of Toxoplasma gondii Dihydrofolate Reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 3694-3699 [PMID:9357537] |
| Dihydrofolate reductase in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2575] [UniProtKB: P00378] | ||||||||
| ChEMBL | Inhibitory activity against chicken liver dihydrofolate reductase | B | 4.33 | pKi | 46773.51 | nM | Ki | J Med Chem (1989) 32: 1895-1905 [PMID:2502631] |
| dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374] | ||||||||
| ChEMBL | Inhibition of human dihydrofolate reductase (DHFR) enzyme | B | 7.23 | pKi | 58.88 | nM | Ki | J Med Chem (1995) 38: 967-972 [PMID:7699713] |
| ChEMBL | Concentration required to inhibit the human Dihydrofolate reductase by 50% was determined | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| dihydrofolate reductase/Dihydrofolate reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2363] [GtoPdb: 2603] [UniProtKB: Q920D2] | ||||||||
| ChEMBL | Inhibitory activity against rat liver dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 4.14 | pIC50 | 73000 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from rat liver | B | 4.48 | pIC50 | 33200 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from rat liver was evaluated using 90 uM dihydrofolic acid as substrate | B | 4.48 | pIC50 | 33200 | nM | IC50 | J Med Chem (1997) 40: 3040-3048 [PMID:9301666] |
| ChEMBL | Inhibition of Dihydrofolate Reductase of Rat Liver. | B | 4.48 | pIC50 | 33200 | nM | IC50 | J Med Chem (1997) 40: 479-485 [PMID:9046338] |
| ChEMBL | Concentration required to inhibit the rat liver Dihydrofolate reductase by 50% was determined | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibition of rat liver Dihydrofolate Reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 3694-3699 [PMID:9357537] |
| Dihydrofolate reductase type 1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2627] [UniProtKB: P00382] | ||||||||
| ChEMBL | Inhibitory activity against Escherichia coli dihydrofolate reductase | B | 7.66 | pKi | 21.88 | nM | Ki | J Med Chem (1991) 34: 46-54 [PMID:1899453] |
ChEMBL data shown on this page come from version 34:
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]
