trimetrexate [Ligand Id: 7613] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL119 (CI-898, Neutrexin, NSC-249008, Trimetrexate, Trimetrexato) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Bifunctional dihydrofolate reductase-thymidylate synthase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163130] [UniProtKB: Q27793] | ||||||||
| ChEMBL | Inhibition of Trypanosoma cruzi DHFR by spectrophotometric assay | B | 8.18 | pKi | 6.6 | nM | Ki | Bioorg Med Chem (2010) 18: 4056-4066 [PMID:20452776] |
| ChEMBL | Inhibition of Trypanosoma cruzi DHFR by spectrophotometric assay | B | 7.69 | pIC50 | 20.2 | nM | IC50 | Bioorg Med Chem (2010) 18: 4056-4066 [PMID:20452776] |
| Dihydrofolate reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1809] [UniProtKB: P0ABQ4] | ||||||||
| ChEMBL | Inhibitory activity against recombinant Escherichia coli dihydrofolate reductase | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2001) 44: 1993-2003 [PMID:11384244] |
| ChEMBL | Inhibition of dihydrofolate reductase in pneumocystis carinii. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1993) 36: 3103-3112 [PMID:8230096] |
| ChEMBL | Inhibition of dihydrofolate reductase from pneumocystis carinii. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2003) 46: 5074-5082 [PMID:14584957] |
| ChEMBL | Inhibitory activity against recombinant Dihydrofolate reductase from Escherichia coli (ecDHFR) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Inhibition of dihydrofolate reductase in Toxoplasma gondii. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1993) 36: 3103-3112 [PMID:8230096] |
| ChEMBL | Inhibition of dihydrofolate reductase from Toxoplasma gondii. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2003) 46: 5074-5082 [PMID:14584957] |
| ChEMBL | Inhibitory activity against Escherichia coli (ec) Dihydrofolate reductase | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| Dihydrofolate reductase in Lactobacillus casei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2902] [UniProtKB: P00381] | ||||||||
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Lactobacillus casei (lcDHFR) | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Lactobacillus casei | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| Dihydrofolate reductase in Mycobacterium avium (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5457] [UniProtKB: O30463] | ||||||||
| ChEMBL | Inhibition of Mycobacterium avium DHFR | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Inhibitory concentration against Mycobacterium avium dihydrofolate reductase | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1811-1815 [PMID:15026078] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Mycobacterium avium (Mycobacterium avium) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2004) 47: 3689-3692 [PMID:15214795] |
| ChEMBL | Concentration required to inhibit the Mycobacterium avium Dihydrofolate reductase by 50% was determined; Range: 1.3-1.7 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibition of Mycobacterium avium DHFR at 37 degC by spectrophotometry | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| Dihydrofolate reductase in Pneumocystis carinii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926] [UniProtKB: P16184] | ||||||||
| ChEMBL | Binding affinity was reported with purified recombinant Pneumocystis carinii Dihydrofolate reductase | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Concentration required to inhibit the Pneumocystis carinii Dihydrofolate reductase by 50% was determined; Range: 34-66 | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibitory concentration against Pneumocystis carinii dihydrofolate reductase | B | 7.33 | pIC50 | 47 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1811-1815 [PMID:15026078] |
| ChEMBL | Compound was tested for inhibition activity against pneumocystis carinii (Pneumocystis carinii) Dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1998) 41: 913-918 [PMID:9526565] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1996) 39: 1271-1280 [PMID:8632434] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii Dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase dihydrofolate reductase from Pneumocystis carinii. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2001) 44: 2391-2402 [PMID:11448221] |
| ChEMBL | Inhibitory activity against purified dihydrofolate reductase from Pneumocystis carinii. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1995) 38: 3660-3668 [PMID:7658454] |
| ChEMBL | Inhibition of dihydrofolate reductase (DHFR) from Pneumocystis carinii(pc) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1999) 42: 2447-2455 [PMID:10395486] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from pneumocystis carinii | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibitory concentration against Pneumocystis carinii Dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 1930-1936 [PMID:9191971] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii (pcDHFR) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Concentration inhibiting Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1995) 38: 2615-2620 [PMID:7629801] |
| ChEMBL | Inhibition against Dihydrofolate reductase in Pneumocystis carinii | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 1173-1177 [PMID:9089339] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Pneumocystis carinii. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | In vitro inhibitory concentration against Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 1886-1893 [PMID:9191966] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from Pneumocystis carinii | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1998) 41: 4533-4541 [PMID:9804692] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii was evaluated using 90 uM dihydrofolic acid as substrate | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 3040-3048 [PMID:9301666] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibition of Dihydrofolate reductase from Pneumocystis carinii (Pneumocystis carinii) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2004) 47: 3689-3692 [PMID:15214795] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 4422-4441 [PMID:23627352] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Pneumocystis carinii (pc) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 470-478 [PMID:9046337] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1997) 40: 3032-3039 [PMID:9301665] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR at 37 degC by spectrophotometry | B | 7.38 | pIC50 | 42 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibition of Pneumocystis carinii (pc) Dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1995) 38: 2158-2165 [PMID:7783147] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1998) 41: 1409-1416 [PMID:9554874] |
| ChEMBL | Inhibition of Dihydrofolate reductase of Pneumocystis carinii | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1994) 37: 4522-4528 [PMID:7799402] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2008) 51: 6195-6200 [PMID:18771252] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR using dihydrofolic acid substrate and NADPH cofactor | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2008) 51: 4589-4600 [PMID:18605720] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase in Pneumocystis carinii at 37 centigrade. | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Inhibitory activity against pneumocystis carinii Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| Dihydrofolate reductase in Candida albicans (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2329] [UniProtKB: P22906] | ||||||||
| ChEMBL | Inhibition of Dihydrofolate reductase enzyme from Candida albicans | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (1996) 39: 892-903 [PMID:8632413] |
| ChEMBL | Inhibition of dihydrofolate reductase in Candida albicans (in vitro). | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1995) 38: 3608-3616 [PMID:7658448] |
| Dihydrofolate reductase in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2425] [UniProtKB: Q07422] | ||||||||
| ChEMBL | Inhibition of Toxoplasma gondii DHFR | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Inhibition of recombinant Dihydrofolate reductase from Toxoplasma gondii (tgDHFR) | B | 5.17 | pIC50 | 6800 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase | B | 5.27 | pIC50 | 5400 | nM | IC50 | J Med Chem (2001) 44: 1993-2003 [PMID:11384244] |
| ChEMBL | Inhibitory concentration against Toxoplasma gondii dihydrofolate reductase | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1811-1815 [PMID:15026078] |
| ChEMBL | Concentration required to inhibit the Toxoplasma gondii Dihydrofolate reductase by 50% was determined; Range: 8-30 | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 1271-1280 [PMID:8632434] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase DHFR from Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2001) 44: 2391-2402 [PMID:11448221] |
| ChEMBL | Inhibitory activity against purified Dihydrofolate reductase from Toxoplasma gondii. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 3660-3668 [PMID:7658454] |
| ChEMBL | Inhibition of dihydrofolate reductase (DHFR) from Toxoplasma gondii(tg) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1999) 42: 2447-2455 [PMID:10395486] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibitory concentration against Toxoplasma gondii Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 1930-1936 [PMID:9191971] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase DHFR in Toxoplasma gondii. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2001) 44: 2555-2564 [PMID:11472209] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii (tgDHFR) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Concentration inhibiting Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 2615-2620 [PMID:7629801] |
| ChEMBL | Inhibition against Dihydrofolate reductase in Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 1173-1177 [PMID:9089339] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Toxoplasma gondii. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | Inhibitory concentration against Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 1886-1893 [PMID:9191966] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 4533-4541 [PMID:9804692] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii was evaluated using 90 uM dihydrofolic acid as substrate | B | 8 | pIC50 | 10 | 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 | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Toxoplasma gondii (Toxoplasma gondii) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2004) 47: 3689-3692 [PMID:15214795] |
| ChEMBL | Inhibition of Toxoplasma gondii (tc) Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 2158-2165 [PMID:7783147] |
| ChEMBL | Inhibition of Toxoplasma gondii Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 1409-1416 [PMID:9554874] |
| ChEMBL | Inhibition of Dihydrofolate reductase of Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1994) 37: 4522-4528 [PMID:7799402] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Toxoplasma gondii (tg) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 470-478 [PMID:9046337] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 3032-3039 [PMID:9301665] |
| ChEMBL | Compound was tested for inhibition activity against Toxoplasma gondii (Toxoplasma gondii) Dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 913-918 [PMID:9526565] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 1836-1845 [PMID:8627607] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2008) 51: 6195-6200 [PMID:18771252] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR at 37 degC by spectrophotometry | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii (tg) Dihydrofolate reductase (DHFR) | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR-TS expressed in Escherichia coli BL21 competent cells using DHF as substrate preincubated for 15 mins followed by substrate and NADPH addition and measured after 60 mins by resazurin dye based diaphorase-coupled assay | B | 8.87 | pIC50 | 1.35 | nM | IC50 | J Med Chem (2019) 62: 1562-1576 [PMID:30624926] |
| dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374] | ||||||||
| ChEMBL | Inhibitory activity against Leu22-Phe mutant human Dihydrofolate reductase | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory compound against Wild-type human DHFR. | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| GtoPdb | In vitro inhibition of wild-type human DHFR | - | 7.89 | pKi | 13 | nM | Ki | J Med Chem (1995) 38: 745-52 [PMID:7877140] |
| ChEMBL | Inhibition of human recombinant Dihydrofolate reductase enzyme | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1996) 39: 892-903 [PMID:8632413] |
| ChEMBL | Inhibition of DHFR (unknown origin) assessed as inhibition constant | B | 10.4 | pKi | 0.04 | nM | Ki | Eur J Med Chem (2021) 211: 113016-113016 [PMID:33243532] |
| ChEMBL | Inhibitory activity against human dihydrofolate reductase | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2001) 44: 1993-2003 [PMID:11384244] |
| ChEMBL | Inhibition of human DHFR by spectrophotometric assay | B | 7.09 | pIC50 | 80.9 | nM | IC50 | Bioorg Med Chem (2010) 18: 4056-4066 [PMID:20452776] |
| ChEMBL | Inhibitory activity against recombinant human Dihydrofolate reductase | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| ChEMBL | Tested for inhibitory concentration against human dihydrofolate reductase(DHFR) | B | 7.91 | pIC50 | 12.2 | nM | IC50 | J Med Chem (1994) 37: 2167-2174 [PMID:8035423] |
| ChEMBL | Inhibition of human recombinant DHFR | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (2013) 56: 4422-4441 [PMID:23627352] |
| ChEMBL | Tested for inhibitory activity against dihydrofolate reductase in human | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1993) 36: 3103-3112 [PMID:8230096] |
| ChEMBL | In vitro inhibition of human dihydrofolate reductase | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (1995) 38: 3608-3616 [PMID:7658448] |
| ChEMBL | Inhibition of human DHFR | B | 9.38 | pIC50 | 0.42 | nM | IC50 | J Med Chem (2021) 64: 17627-17655 [PMID:34894691] |
| dihydrofolate reductase/Dihydrofolate reductase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4564] [GtoPdb: 2603] [UniProtKB: P00375] | ||||||||
| ChEMBL | Inhibitory constant for F31A/F34A murine dihydrofolate reductase (DHFR) | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2003) 46: 2816-2818 [PMID:12825924] |
| ChEMBL | Inhibitory constant for murine Wild-type dihydrofolate reductase (DHFR) | B | 10.22 | pKi | 0.06 | nM | Ki | J Med Chem (2003) 46: 2816-2818 [PMID:12825924] |
| dihydrofolate reductase/Dihydrofolate reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2363] [GtoPdb: 2603] [UniProtKB: Q920D2] | ||||||||
| ChEMBL | Inhibition of rat liver DHFR | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Inhibitory activity against rat dihydrofolate reductase | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1811-1815 [PMID:15026078] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase DHFR from rat liver. | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2001) 44: 2391-2402 [PMID:11448221] |
| ChEMBL | Concentration required to inhibit the rat liver Dihydrofolate reductase by 50% was determined; Range: 7.0-9.2 | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibitory activity against rat liver dihydrofolate reductase. | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1996) 39: 1836-1845 [PMID:8627607] |
| ChEMBL | Inhibition of rat liver dihydrofolate reductase. | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1993) 36: 3103-3112 [PMID:8230096] |
| ChEMBL | Inhibitory activity against rat liver dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1996) 39: 1271-1280 [PMID:8632434] |
| ChEMBL | Inhibitory activity against rat liver Dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory activity against purified dihydrofolate reductase from rat | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 3660-3668 [PMID:7658454] |
| ChEMBL | Inhibition of dihydrofolate reductase (DHFR) from rat liver (rl) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1999) 42: 2447-2455 [PMID:10395486] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | Inhibitory concentration against Rat liver Dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 1930-1936 [PMID:9191971] |
| ChEMBL | Inhibition of dihydrofolate reductase from rat liver. | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 5074-5082 [PMID:14584957] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase DHFR in rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2001) 44: 2555-2564 [PMID:11472209] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from rat liver (rlDHFR) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Concentration inhibiting rat liver dihydrofolate reductase. | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 2615-2620 [PMID:7629801] |
| ChEMBL | Inhibition against Dihydrofolate reductase in rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 1173-1177 [PMID:9089339] |
| ChEMBL | Inhibition of rat liver dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | In vitro inhibitory concentration against rat liver dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 1886-1893 [PMID:9191966] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 4533-4541 [PMID:9804692] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from rat liver was evaluated using 90 uM dihydrofolic acid as substrate | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 3040-3048 [PMID:9301666] |
| ChEMBL | Inhibitory activity against rat liver dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2004) 47: 3689-3692 [PMID:15214795] |
| ChEMBL | Inhibition of rat liver Dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 2158-2165 [PMID:7783147] |
| ChEMBL | Inhibition of Dihydrofolate reductase of rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 1409-1416 [PMID:9554874] |
| ChEMBL | Inhibition of Dihydrofolate reductase (DHFR) of in rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1994) 37: 4522-4528 [PMID:7799402] |
| ChEMBL | Inhibition of rat liver dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2008) 51: 6195-6200 [PMID:18771252] |
| ChEMBL | Inhibition of rat liver DHFR using dihydrofolic acid substrate and NADPH cofactor | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2008) 51: 4589-4600 [PMID:18605720] |
| ChEMBL | Inhibition of rat liver DHFR at 37 degC by spectrophotometry | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from rat liver | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibition of rat liver DHFR | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2013) 56: 4422-4441 [PMID:23627352] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Rat liver (rl) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 470-478 [PMID:9046337] |
| ChEMBL | Inhibition of rat liver dihydrofolate reductase | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 3032-3039 [PMID:9301665] |
| ChEMBL | Compound was tested for inhibition activity against rat liver lipophilic Dihydrofolate reductase (DHFR). | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 913-918 [PMID:9526565] |
| Dihydrofolate reductase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2576] [UniProtKB: P07807] | ||||||||
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase. | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (1996) 39: 1836-1845 [PMID:8627607] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium falciparum isolate Kil-164 expressing DHFR Ser108Asn, Asn51Ile, Cys59Arg and Ile164Leu quadruple mutant by [3H]hypoxanthine incorporation assay | F | 7.35 | pIC50 | 44.66 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn and Cys59Arg or Ser108Asn and Asn51Ile double mutant by [3H]hypoxanthine incorporation assay | F | 7.39 | pIC50 | 40.92 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Kenyan isolates by [3H]hypoxanthine incorporation assay | F | 7.52 | pIC50 | 30 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum V1S expressing DHFR quadruple mutant with point mutations at codons 108, 51, 59 and 164 gene by [3H]hypoxanthine incorporation assay | F | 7.61 | pIC50 | 24.8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn, Asn51Ile and Cys59Arg triple mutant by [3H]hypoxanthine incorporation assay | F | 7.68 | pIC50 | 20.91 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against pyrimethamine-sensitive Plasmodium falciparum 3D7 expressing wild type DHFR by [3H]hypoxanthine incorporation assay | F | 8.72 | pIC50 | 1.9 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
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]
