trimethoprim [Ligand Id: 10931] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL22 (BW 56-72, BW-56-72, Infectotrimet, Ipral, Ledatrim, Monotrim, NIH-204, NSC-106568, Polytrim, Primsol, Proloprim, Proloprin, Syraprim, TCMDC-125538, Tiempe, Trimethoprim, Trimethoprimum, Trimogal, Trimopan, Trimpex, Trimpex 200, Triprimix 200, Wellcoprim) |
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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 | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2002) 45: 233-241 [PMID:11754594] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase in Neisseria gonorrhoeae | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1989) 32: 1927-1935 [PMID:2502632] |
| Bifunctional dihydrofolate reductase-thymidylate synthase in Cryptosporidium parvum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366489] [UniProtKB: Q27552] | ||||||||
| ChEMBL | Inhibition of Cryptosporidium hominis DHFR | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4366-4370 [PMID:16750361] |
| ChEMBL | Inhibition of Cryptosporidium parvum recombinant DHFR using dihydrofolate as substrate incubated for 5 min prior to substrate addition by spectrophotometric assay | B | 5.4 | pIC50 | 4000 | nM | IC50 | Med Chem Res (2008) 17: 541-563 |
| Dihydrofolate reductase in Neisseria gonorrhoeae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3565] [UniProtKB: P04174] | ||||||||
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) of Neisseria gonorrhoea | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1987) 30: 348-356 [PMID:3100802] |
| ChEMBL | Inhibitory activity against Neisseria gonorrhoeae dihydrofolate reductase at 10e8 M | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1991) 34: 550-555 [PMID:1995876] |
| Dihydrofolate reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1809] [UniProtKB: P0ABQ4] | ||||||||
| ChEMBL | Inhibition constant against Dihydrofolate reductase | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2493-2496 [PMID:12852950] |
| ChEMBL | Inhibition constant against binding of Escherichia coli dihydrofolate reductase | B | 8.87 | pKi | 1.35 | nM | Ki | J Med Chem (1988) 31: 1396-1406 [PMID:3290487] |
| ChEMBL | Antibacterial activity against Escherichia coli | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Binding affinity against Dihydrofolate reductase of Escherichia coli | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1985) 28: 303-311 [PMID:3973902] |
| ChEMBL | Binding affinity for Escherichia coli Dihydrofolate reductase | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1982) 25: 1120-1122 [PMID:6754932] |
| ChEMBL | Apparent binding affinity against Dihydrofolate reductase in Escherichia coli | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1989) 32: 1942-1949 [PMID:2666668] |
| ChEMBL | Inhibition of recombinant Escherichia coli DHFR expressed in Escherichia coli BL21(DE3) cells assessed as reduction in NADPH oxidation using dihydrofolate as substrate preincubated for 5 mins followed by substrate addition | B | 9.66 | pKi | 0.22 | nM | Ki | ACS Med Chem Lett (2016) 7: 692-696 [PMID:27437079] |
| ChEMBL | In vitro inhibition of Escherichia coli (B41) Dihydrofolate reductase. | B | 2 | pIC50 | 10000000 | nM | IC50 | J Med Chem (1990) 33: 434-444 [PMID:2404122] |
| ChEMBL | Inhibition of dihydrofolate reductase from pneumocystis carinii. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2003) 46: 5074-5082 [PMID:14584957] |
| ChEMBL | Inhibition of dihydrofolate reductase from Toxoplasma gondii. | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2003) 46: 5074-5082 [PMID:14584957] |
| ChEMBL | Inhibitory activity against recombinant Escherichia coli dihydrofolate reductase | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2001) 44: 1993-2003 [PMID:11384244] |
| ChEMBL | Inhibition of Escherichia coli Dihydrofolate reductase in presence of 100 uM Dihydrofolate reductase | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2493-2496 [PMID:12852950] |
| ChEMBL | Inhibition of Escherichia coli DHFR | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2010) 53: 1563-1578 [PMID:20092323] |
| ChEMBL | Inhibition of Escherichia coli dihydrofolate reductase | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2008) 51: 4589-4600 [PMID:18605720] |
| ChEMBL | Inhibitory activity against Escherichia coli (ec) Dihydrofolate reductase | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| ChEMBL | Inhibition of Escherichia coli Dihydrofolate reductase in presence of 30 uM Dihydrofolate reductase | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2493-2496 [PMID:12852950] |
| ChEMBL | Inhibitory activity against recombinant Dihydrofolate reductase from Escherichia coli (ecDHFR) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Compound was evaluated as inhibitor of Escherichia coli Dihydrofolate reductase | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2003) 46: 591-600 [PMID:12570380] |
| ChEMBL | Inhibition of Escherichia coli DHFR | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2012) 20: 4217-4225 [PMID:22739090] |
| ChEMBL | Inhibition of Escherichia coli DHFR | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2008) 51: 5789-5797 [PMID:18800768] |
| ChEMBL | Inhibition of Escherichia coli dihydrofolate reductase | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2009) 52: 4892-4902 [PMID:19719239] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from Escherichia coli | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1987) 30: 348-356 [PMID:3100802] |
| ChEMBL | Inhibition of Escherichia coli dihydrofolate reductase (DHFR) enzyme by Iclaprim | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
| ChEMBL | Inhibitory activity against Escherichia coli dihydrofolate reductase at 10e8 M | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1991) 34: 550-555 [PMID:1995876] |
| ChEMBL | In vitro inhibition of dihydrofolate reductase of Escherichia coli | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Compound was tested for inhibition of Escherichia coli Dihydrofolate reductase. | B | 8.23 | pIC50 | 5.89 | nM | IC50 | J Med Chem (1996) 39: 4825-4832 [PMID:8941396] |
| ChEMBL | In vitro inhibition of Escherichia coli dihydrofolate reductase. | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase in Escherichia coli | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1989) 32: 1936-1942 [PMID:2502633] |
| ChEMBL | Inhibition against dihydrofolate reductase enzyme of Escherichia coli | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1980) 23: 535-541 [PMID:6991695] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase of Escherichia coli | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1981) 24: 933-941 [PMID:7035668] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) enzyme from Escherichia coli | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1987) 30: 1998-2004 [PMID:3312605] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase enzyme purified from Escherichia coli | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1980) 23: 379-384 [PMID:6991692] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase obtained from E. coli; Range 0.005-0.007 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1991) 34: 1383-1394 [PMID:2016714] |
| Dihydrofolate reductase in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1681620] [UniProtKB: P0A017] | ||||||||
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus recombinant DHFR F98Y/H149R double mutant expressed in Escherichia coli BL21 (DE3) cells assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 5.76 | pKi | 1729 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus recombinant DHFR H30N/F98Y double mutant expressed in Escherichia coli BL21 (DE3) cells assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 6.23 | pKi | 595.1 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus recombinant DHFR H149R mutant expressed in Escherichia coli BL21 (DE3) cells assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 6.62 | pKi | 240.8 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Inhibition of TMP-resistant Staphylococcus aureus DHFR F99Y mutant assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 7.05 | pKi | 90 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
| ChEMBL | Inhibition of Staphylococcus aureus DHFR F98Y mutant by MTS assay | B | 7.27 | pKi | 53.6 | nM | Ki | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus recombinant DHFR F98Y mutant expressed in Escherichia coli BL21 (DE3) cells assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 7.83 | pKi | 14.68 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus recombinant DHFR H30N mutant expressed in Escherichia coli BL21 (DE3) cells assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 8.16 | pKi | 6.89 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Antibacterial activity against Staphylococcus aureus | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay | B | 8.36 | pKi | 4.4 | nM | Ki | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
| ChEMBL | Inhibition of TMP/methicillin-resistant Staphylococcus aureus wild type DHFR assessed as oxidation of NADPH pre-incubated for 5 mins followed by dihydrofolate substrate addition | B | 8.46 | pKi | 3.43 | nM | Ki | J Med Chem (2016) 59: 6493-6500 [PMID:27308944] |
| ChEMBL | Inhibition of recombinant Staphylococcus aureus DHFR expressed in Escherichia coli BL21(DE3) cells assessed as reduction in NADPH oxidation using dihydrofolate as substrate preincubated for 5 mins followed by substrate addition | B | 8.46 | pKi | 3.43 | nM | Ki | ACS Med Chem Lett (2016) 7: 692-696 [PMID:27437079] |
| ChEMBL | Inhibition of Staphylococcus aureus DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 8.91 | pKi | 1.24 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
| ChEMBL | Inhibition of Staphylococcus aureus DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2014) 57: 651-668 [PMID:24428639] |
| ChEMBL | Inhibition of trimethoprim-resistant Staphylococcus aureus DHFR F98Y mutant | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (2007) 50: 4374-4381 [PMID:17696333] |
| ChEMBL | Tested for inhibition of TMP-Resistant Dihydrofolate reductase from Staphylococcus aureus 157/4696. | B | 4.72 | pIC50 | 19000 | nM | IC50 | J Med Chem (2003) 46: 2304-2312 [PMID:12773035] |
| ChEMBL | Inhibition of trimethoprim-resistant Staphylococcus aureus DfrB type dihydrofolate reductase F98Y mutant | B | 4.99 | pIC50 | 10243 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3620-3627 [PMID:19546364] |
| ChEMBL | Inhibition of methicillin-resistant Staphylococcus aureus DHFR F98Y mutant | B | 5.77 | pIC50 | 1700 | nM | IC50 | Medchemcomm (2013) 4: 908-915 |
| ChEMBL | Inhibition of Staphylococcus aureus DHFR F98Y mutant by MTS assay | B | 6.27 | pIC50 | 539.7 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
| ChEMBL | Antibacterial activity against TMP-Resistant Dihydrofolate reductase from Staphylococcus aureus 157/4696 | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2003) 46: 2304-2312 [PMID:12773035] |
| ChEMBL | Inhibition of methicillin-resistant Staphylococcus aureus DHFR | B | 7.64 | pIC50 | 23 | nM | IC50 | Medchemcomm (2013) 4: 908-915 |
| ChEMBL | Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay | B | 7.84 | pIC50 | 14.4 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
| ChEMBL | Inhibition of Staphylococcus aureus dihydrofolate reductase (DHFR) enzyme by Iclaprim | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
| Dihydrofolate reductase in Bacillus anthracis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5270] [UniProtKB: Q81R22] | ||||||||
| ChEMBL | Inhibition of wild type Bacillus anthracis recombinant DHFR | B | 4.62 | pKi | 24100 | nM | Ki | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| ChEMBL | Inhibition of Bacillus anthracis recombinant DHFR F96I mutant | B | 4.86 | pKi | 13700 | nM | Ki | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| ChEMBL | Inhibition of Bacillus anthracis recombinant DHFR Y102F mutant | B | 6.32 | pKi | 480 | nM | Ki | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| ChEMBL | Inhibition of Bacillus anthracis DHFR | B | 4.11 | pIC50 | 77000 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3065-3073 [PMID:19364848] |
| ChEMBL | Inhibition of wild type Bacillus anthracis recombinant DHFR | B | 4.15 | pIC50 | 71400 | nM | IC50 | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| ChEMBL | Inhibition of Bacillus anthracis recombinant DHFR expressed in mouse M15 cells assessed as rate of enzyme-dependent NADPH oxidation | B | 4.15 | pIC50 | 71000 | nM | IC50 | J Med Chem (2008) 51: 7532-7540 [PMID:19007108] |
| ChEMBL | Inhibition of Bacillus anthracis recombinant DHFR F96I mutant | B | 5.24 | pIC50 | 5760 | nM | IC50 | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| ChEMBL | Inhibition of Bacillus anthracis recombinant DHFR Y102F mutant | B | 5.42 | pIC50 | 3780 | nM | IC50 | J Med Chem (2010) 53: 7327-7336 [PMID:20882962] |
| Dihydrofolate reductase in Lactobacillus casei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2902] [UniProtKB: P00381] | ||||||||
| ChEMBL | Inhibitory activity against Lactobacillus casei dihydrofolate reductase | B | 6.88 | pKi | 131.83 | nM | Ki | J Med Chem (1989) 32: 1895-1905 [PMID:2502631] |
| ChEMBL | Compound was evaluated as inhibitor of Lactobacillus casei Dihydrofolate reductase | B | 6.21 | pIC50 | 620 | nM | IC50 | J Med Chem (2003) 46: 591-600 [PMID:12570380] |
| ChEMBL | Inhibition of Lactobacillus casei DHFR | B | 6.21 | pIC50 | 620 | nM | IC50 | J Med Chem (2007) 50: 3283-3289 [PMID:17569517] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Lactobacillus casei | B | 6.99 | pIC50 | 103 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Lactobacillus casei (lcDHFR) | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| Dihydrofolate reductase in Mycobacterium avium (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5457] [UniProtKB: O30463] | ||||||||
| ChEMBL | Inhibition of Mycobacterium avium DHFR | B | 3.52 | pIC50 | 300000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Concentration required to inhibit the Mycobacterium avium Dihydrofolate reductase by 50% was determined; Range: 260-350 | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibition of Mycobacterium avium DHFR at 37 degC by spectrophotometry | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibition of Dihydrohydrofolate reductase(DHFR) of Mycobacterium avium | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2003) 46: 1726-1736 [PMID:12699390] |
| ChEMBL | Inhibitory concentration against Mycobacterium avium DHFR | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2005) 48: 4420-4431 [PMID:15974594] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase of Mycobacterium avium | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2004) 47: 1475-1486 [PMID:14998335] |
| ChEMBL | Inhibition of partially purified dihydrofolate reductase (DHFR) from Mycobacterium avium (Ma) | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2002) 45: 233-241 [PMID:11754594] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Mycobacterium avium | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | Inhibition of Mycobacterium avium DHFR | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2007) 50: 3283-3289 [PMID:17569517] |
| Dihydrofolate reductase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6065] [UniProtKB: P9WNX1] | ||||||||
| ChEMBL | Inhibition of recombinant Mycobacterium tuberculosis DHFR expressed in Escherichia coli BL21(DE3) cells using DHF as substrate and NADPH as cofactor by fluorimetric analysis | B | 4.06 | pIC50 | 88000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115600-115600 [PMID:32631571] |
| 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 | 6.82 | pKi | 152 | nM | Ki | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Inhibition of dihydrofolate reductase (DHFR) from Pneumocystis carinii. | B | 6.82 | pKi | 151.36 | nM | Ki | J Med Chem (1995) 38: 967-972 [PMID:7699713] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 1.92 | pIC50 | 12000000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase (DHFR) enzyme by Iclaprim | B | 4.37 | pIC50 | 43000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
| ChEMBL | Inhibitory concentration against Pneumocystis carinii dihydrofolate reductases (DHFR) | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase dihydrofolate reductase from Pneumocystis carinii. | B | 4.57 | pIC50 | 26800 | nM | IC50 | J Med Chem (2001) 44: 2391-2402 [PMID:11448221] |
| ChEMBL | Inhibitory activity against pneumocystis carinii Dihydrofolate reductase | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| ChEMBL | Inhibitory concentration against Pneumocystis carinii DHFR | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2005) 48: 4420-4431 [PMID:15974594] |
| ChEMBL | Inhibition of Dihydrohydrofolate reductase(DHFR) of Pneumocystis carinii | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2003) 46: 1726-1736 [PMID:12699390] |
| ChEMBL | Concentration required to inhibit the Pneumocystis carinii Dihydrofolate reductase by 50% was determined; Range: 10000-16000 | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 4.9 | pIC50 | 12500 | nM | IC50 | J Med Chem (2013) 56: 4422-4441 [PMID:23627352] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | The ability to inhibit Pneumocystis carinii Dihydrofolate reductase was tested | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1999) 42: 1007-1017 [PMID:10090784] |
| ChEMBL | Concentration inhibiting Pneumocystis carinii dihydrofolate reductase. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 2615-2620 [PMID:7629801] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii (pcDHFR) | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Inhibition against Dihydrofolate reductase in Pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1997) 40: 1173-1177 [PMID:9089339] |
| ChEMBL | Inhibition of Pneumocystis carinii Dihydrofolate Reductase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1997) 40: 3694-3699 [PMID:9357537] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from Pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1998) 41: 4533-4541 [PMID:9804692] |
| ChEMBL | Inhibition of Dihydrofolate Reductase of Pneumocystis carinii. | B | 4.92 | pIC50 | 12000 | 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 | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibition of Pneumocystis carinii (pc) Dihydrofolate reductase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 2158-2165 [PMID:7783147] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1998) 41: 1409-1416 [PMID:9554874] |
| ChEMBL | Inhibition of Dihydrofolate reductase of Pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1994) 37: 4522-4528 [PMID:7799402] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4366-4370 [PMID:16750361] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2007) 50: 3283-3289 [PMID:17569517] |
| ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase | B | 4.92 | pIC50 | 12000 | 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 | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2008) 51: 4589-4600 [PMID:18605720] |
| ChEMBL | Inhibition of Pneumocystis carinii DHFR at 37 degC by spectrophotometry | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Pneumocystis carinii. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Pneumocystis carinii (pc) | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1997) 40: 470-478 [PMID:9046337] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase in Pneumocystis carinii at 37 centigrade. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 4739-4759 [PMID:7490723] |
| ChEMBL | Compound was tested for inhibition activity against Dihydrofolate reductase in pneumocystis carinii (Pneumocystis carinii). | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1998) 41: 913-918 [PMID:9526565] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1996) 39: 1271-1280 [PMID:8632434] |
| ChEMBL | Inhibitory activity against Pneumocystis carinii Dihydrofolate reductase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductace enzyme of Pneumocystis carinii | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2004) 47: 1475-1486 [PMID:14998335] |
| ChEMBL | Inhibitory activity against purified DHFR (Dihydrofolate reductase) from Pneumocystis carinii. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1995) 38: 3660-3668 [PMID:7658454] |
| ChEMBL | The compound was tested for inhibition of dihydrofolate reductase(DHFR) from Pneumocystis carinii(pc) | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1999) 42: 2447-2455 [PMID:10395486] |
| ChEMBL | Concentration required to inhibit the Pneumocystis carinii Dihydrofolate reductase by 50% was determined (reported by workers at Hoffman-LaRoche) | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| Dihydrofolate reductase in Candida albicans (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2329] [UniProtKB: P22906] | ||||||||
| ChEMBL | Inhibition of dihydrofolate reductase in Candida albicans (in vitro). | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1995) 38: 3608-3616 [PMID:7658448] |
| ChEMBL | Inhibition of Candida albicans DHFR expressed in Escherichia coli BL21 (DE3) assessed as rate of NADPH consumption using dihydrofolate as substrate | B | 4.38 | pIC50 | 42000 | nM | IC50 | Bioorg Med Chem (2009) 17: 4866-4872 [PMID:19560363] |
| ChEMBL | Inhibition of Candida albicans DHFR | B | 4.39 | pIC50 | 41000 | nM | IC50 | Medchemcomm (2013) 4: 908-915 |
| ChEMBL | Inhibitory activity against cell free dihydrofolate reductase (DHFR) from Candida albicans | B | 4.52 | pIC50 | 30300 | nM | IC50 | J Med Chem (2004) 47: 240-253 [PMID:14695838] |
| ChEMBL | Inhibitory activity against cell free dihydrofolate reductase (DHFR) from Mycobacterium lufu | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2004) 47: 240-253 [PMID:14695838] |
| ChEMBL | Inhibitory activity against cell free dihydrofolate reductase (DHFR) from Escherichia coli | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2004) 47: 240-253 [PMID:14695838] |
| Dihydrofolate reductase in Leishmania major (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4614] [UniProtKB: P07382] | ||||||||
| ChEMBL | Inhibition of Leishmania major DHFR assessed by NADPH oxidation measured by spectrophotometric method | B | 6.92 | pKi | 120 | nM | Ki | Eur J Med Chem (2021) 210: 112986-112986 [PMID:33187806] |
| ChEMBL | Inhibition of Leishmania major DHFR in promastigote stage Leishmania major using dihydrofolic acid as substrate in presence of NADPH measured after 5 days by spectrophotometric method | B | 4.69 | pIC50 | 20500 | nM | IC50 | Eur J Med Chem (2021) 210: 112986-112986 [PMID:33187806] |
| Dihydrofolate reductase in Toxoplasma gondii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2425] [UniProtKB: Q07422] | ||||||||
| ChEMBL | Inhibition of Toxoplasma gondii DHFR | B | 2.55 | pIC50 | 2800000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| 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 | 4.48 | pIC50 | 33100 | nM | IC50 | J Med Chem (2019) 62: 1562-1576 [PMID:30624926] |
| ChEMBL | Inhibitory concentration against Toxoplasma gondii dihydrofolate reductases (DHFR) | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR-TS | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2007) 50: 940-950 [PMID:17269758] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR | B | 5.17 | pIC50 | 6800 | nM | IC50 | Bioorg Med Chem (2012) 20: 4217-4225 [PMID:22739090] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR | B | 5.17 | pIC50 | 6800 | nM | IC50 | J Med Chem (2008) 51: 5789-5797 [PMID:18800768] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 5.17 | pIC50 | 6800 | nM | IC50 | J Med Chem (2009) 52: 4892-4902 [PMID:19719239] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Med Chem (2001) 44: 1993-2003 [PMID:11384244] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii (tg) Dihydrofolate reductase (DHFR) | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2002) 45: 5173-5181 [PMID:12408727] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2008) 51: 4589-4600 [PMID:18605720] |
| ChEMBL | Inhibitory activity against Dihydrohydrofolate reductase(DHFR) of Toxoplasma gondii | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2003) 46: 1726-1736 [PMID:12699390] |
| ChEMBL | Concentration required to inhibit the Toxoplasma gondii Dihydrofolate reductase by 50% was determined; Range: 2400-3300 | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR at 37 degC by spectrophotometry | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem (2010) 18: 953-961 [PMID:20056546] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase of Toxoplasma gondii | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2004) 47: 1475-1486 [PMID:14998335] |
| ChEMBL | Inhibitory concentration against Toxoplasma gondii DHFR | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2005) 48: 4420-4431 [PMID:15974594] |
| ChEMBL | Inhibition of Toxoplasma gondii DHFR | B | 5.56 | pIC50 | 2730 | nM | IC50 | J Med Chem (2007) 50: 3283-3289 [PMID:17569517] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase | B | 5.56 | pIC50 | 2730 | nM | IC50 | J Med Chem (1996) 39: 1271-1280 [PMID:8632434] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase (in 90 uM dihydrofolic acid) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1996) 39: 1438-1446 [PMID:8691474] |
| ChEMBL | Inhibition of Toxoplasma gondii (tc) Dihydrofolate reductase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 2158-2165 [PMID:7783147] |
| ChEMBL | Inhibition of Toxoplasma gondii Dihydrofolate reductase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1998) 41: 1409-1416 [PMID:9554874] |
| ChEMBL | Inhibition of partially purified dihydrofolate reductase (DHFR) from Toxoplasma gondii (Tg) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2002) 45: 233-241 [PMID:11754594] |
| ChEMBL | Inhibition of Dihydrofolate reductase of Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1994) 37: 4522-4528 [PMID:7799402] |
| ChEMBL | Inhibition of Toxoplasma gondii dihydrofolate reductase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2008) 51: 6195-6200 [PMID:18771252] |
| ChEMBL | Inhibitory activity against DHFR (Dihydrofolate reductase) from Toxoplasma gondii. | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1999) 42: 4853-4860 [PMID:10579848] |
| ChEMBL | Inhibitory concentration against Dihydrofolate reductase from Toxoplasma gondii (tg) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 470-478 [PMID:9046337] |
| ChEMBL | Compound was tested for inhibition activity against Dihydrofolate reductase in Toxoplasma gondii (Toxoplasma gondii) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1998) 41: 913-918 [PMID:9526565] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii dihydrofolate reductase. | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1996) 39: 1836-1845 [PMID:8627607] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductase DHFR from Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2001) 44: 2391-2402 [PMID:11448221] |
| ChEMBL | Inhibitory activity against Toxoplasma gondii Dihydrofolate reductase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 745-752 [PMID:7877140] |
| ChEMBL | Inhibitory activity against purified DHFR (Dihydrofolate reductase) from Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 3660-3668 [PMID:7658454] |
| ChEMBL | The compound was tested for inhibition of dihydrofolate reductase(DHFR) from Toxoplasma gondii(tg) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1999) 42: 2447-2455 [PMID:10395486] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase from Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1998) 41: 1263-1271 [PMID:9548816] |
| ChEMBL | The ability to inhibit Toxoplasma gondii Dihydrofolate reductase was tested | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1999) 42: 1007-1017 [PMID:10090784] |
| ChEMBL | Concentration inhibiting Toxoplasma gondii dihydrofolate reductase. | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 2615-2620 [PMID:7629801] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii (tgDHFR) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| ChEMBL | Inhibition against Dihydrofolate reductase in Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 1173-1177 [PMID:9089339] |
| ChEMBL | Inhibition of Toxoplasma gondii Dihydrofolate Reductase | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 3694-3699 [PMID:9357537] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 1778-1785 [PMID:7752201] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) from Toxoplasma gondii | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1998) 41: 4533-4541 [PMID:9804692] |
| ChEMBL | Inhibition of Dihydrofolate Reductase of Toxoplasma gondii. | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 479-485 [PMID:9046338] |
| ChEMBL | Inhibitory activity against recombinant Dihydrofolate reductase from Toxoplasma gondii (tgDHFR) | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| Dihydrofolate reductase in Plasmodium berghei str. ANKA (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3963] [UniProtKB: Q27713] | ||||||||
| ChEMBL | In vitro inhibition of dihydrofolate reductase of Plasmodium berghei | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) of Plasmodium berghei | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1987) 30: 348-356 [PMID:3100802] |
| ChEMBL | Compound was tested for its inhibition against dihydrofolate reductase enzyme of Plasmodium berghei | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1980) 23: 535-541 [PMID:6991695] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) enzyme from Plasmodium berghei | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1987) 30: 1998-2004 [PMID:3312605] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase enzyme purified from Plasmodium berghei. | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1980) 23: 379-384 [PMID:6991692] |
| Dihydrofolate reductase in Plasmodium falciparum K1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1939] [UniProtKB: P13922] | ||||||||
| ChEMBL | Inhibitory activity against quadruple mutant dihydrofolate reductase (N51I C59R S108N I164L DHFR) | B | 5.18 | pKi | 6664.5 | nM | Ki | J Med Chem (2004) 47: 345-354 [PMID:14711307] |
| ChEMBL | Inhibitory activity against triple mutant dihydrofolate reductase (C59R S108 NI164L DHFR) | B | 5.24 | pKi | 5688.7 | nM | Ki | J Med Chem (2004) 47: 345-354 [PMID:14711307] |
| ChEMBL | Inhibitory activity against double mutant dihydrofolate reductase (C59R+S108N DHFR) | B | 6.62 | pKi | 242.1 | nM | Ki | J Med Chem (2004) 47: 345-354 [PMID:14711307] |
| ChEMBL | Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) | B | 6.62 | pKi | 242.1 | nM | Ki | J Med Chem (2002) 45: 1244-1252 [PMID:11881993] |
| ChEMBL | Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) | B | 6.88 | pKi | 132.3 | nM | Ki | J Med Chem (2002) 45: 1244-1252 [PMID:11881993] |
| ChEMBL | Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR) | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (2004) 47: 345-354 [PMID:14711307] |
| ChEMBL | Inhibition of the wild-type dihydrofolate reductase (DHFR) | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (2002) 45: 1244-1252 [PMID:11881993] |
| ChEMBL | Inhibition of Plasmodium falciparum DHFR | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4366-4370 [PMID:16750361] |
| dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374] | ||||||||
| ChEMBL | Inhibition of human DHFR | B | 4.32 | pKi | 48000 | nM | Ki | Eur J Med Chem (2017) 135: 467-478 [PMID:28477572] |
| ChEMBL | Inhibition of recombinant human DHFR assessed as reduction in NADPH oxidation using dihydrofolate as substrate preincubated for 5 mins followed by substrate addition | B | 4.34 | pKi | 45783.5 | nM | Ki | ACS Med Chem Lett (2016) 7: 692-696 [PMID:27437079] |
| ChEMBL | Inhibition of human DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 4.72 | pKi | 19070 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
| ChEMBL | Inhibition of human DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH | B | 4.72 | pKi | 19070 | nM | Ki | J Med Chem (2014) 57: 651-668 [PMID:24428639] |
| ChEMBL | Inhibition of human DHFR in presence of variable DHFA level by enzyme kinetics assay | B | 5.31 | pKi | 4900 | nM | Ki | Bioorg Med Chem (2009) 17: 7324-7336 [PMID:19748785] |
| ChEMBL | Inhibition of recombinant Dihydrofolate reductase from humans. | B | 5.86 | pKi | 1380 | nM | Ki | J Med Chem (1999) 42: 4300-4312 [PMID:10543874] |
| ChEMBL | Inhibition of recombinant Dihydrofolate reductase from Trypanosoma cruzi. | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (1999) 42: 4300-4312 [PMID:10543874] |
| ChEMBL | Inhibition of human dihydrofolate reductase (DHFR) enzyme | B | 6.71 | pKi | 194.98 | nM | Ki | J Med Chem (1995) 38: 967-972 [PMID:7699713] |
| ChEMBL | Inhibition of recombinant Dihydrofolate reductase from Leishmania major. | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (1999) 42: 4300-4312 [PMID:10543874] |
| ChEMBL | Inhibition of recombinant Dihydrofolate reductase from humans. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1999) 42: 4300-4312 [PMID:10543874] |
| ChEMBL | Inhibition of human DHFR assessed as NADPH consumption for conversion of dihydrofolic acid to tetrahydrofolic acid after 6 mins every 5 sec by UV-Visible Spectrophotometer method | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5428-5431 [PMID:21788136] |
| ChEMBL | Inhibitory activity against TMP-susceptible Dihydrofolate reductase from Staphylococcus pneumoniae ATCC 49619 | B | 4.47 | pIC50 | 34000 | nM | IC50 | J Med Chem (2003) 46: 2304-2312 [PMID:12773035] |
| ChEMBL | Inhibition of human recombinant DHFR | B | 4.49 | pIC50 | 32200 | nM | IC50 | J Med Chem (2013) 56: 4422-4441 [PMID:23627352] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductace enzyme of Cryptosporidium parvum of human origin | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2004) 47: 1475-1486 [PMID:14998335] |
| ChEMBL | Compound was evaluated as inhibitor of human Dihydrofolate reductase | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2003) 46: 591-600 [PMID:12570380] |
| ChEMBL | Antibacterial activity against TMP-susceptible Dihydrofolate reductase from Staphylococcus pneumoniae ATCC 49619 | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2003) 46: 2304-2312 [PMID:12773035] |
| ChEMBL | Inhibitory concentration against dihydrofolate reductace enzyme of Cryptosporidium parvum of bovine origin | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2004) 47: 1475-1486 [PMID:14998335] |
| ChEMBL | Concentration required to inhibit the human Dihydrofolate reductase by 50% was determined (reported by workers at Hoffman-LaRoche) | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2004) 47: 2475-2485 [PMID:15115391] |
| ChEMBL | In vitro inhibition of dihydrofolate reductase of Neisseria gonorrhoeae | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase in Neisseria gonorrhoeae | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1989) 32: 1936-1942 [PMID:2502633] |
| ChEMBL | Inhibitory activity against dihydrofolate reductase (DHFR) enzyme from Neisseria gonorrhoeae | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1987) 30: 1998-2004 [PMID:3312605] |
| ChEMBL | Inhibition of Neisseria gonorrhoeae Dihydrofolate reductase(DHFR) | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1988) 31: 122-129 [PMID:3121854] |
| ChEMBL | Inhibition of DHFR using dihydrofolate as substrate following 3 mins substrate preincubation measured after 3 mins by spectrophotometric analysis | B | 6.91 | pIC50 | 123 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2428-2433 [PMID:22406152] |
| ChEMBL | Inhibitory activity against TMP-susceptible DHFR from Staphylococcus pneumoniae ATCC 49619 | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2003) 46: 2304-2312 [PMID:12773035] |
| ChEMBL | Inhibition of Streptococcus pneumoniae dihydrofolate reductase (DHFR) enzyme by Iclaprim | B | 7.12 | pIC50 | 75 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
| ChEMBL | Inhibitory activity against Dihydrofolate reductase from recombinant human (hDHFR) | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1998) 41: 3426-3434 [PMID:9719595] |
| dihydrofolate reductase/Dihydrofolate reductase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4564] [GtoPdb: 2603] [UniProtKB: P00375] | ||||||||
| ChEMBL | Competitive inhibition of mouse DHFR by enzyme kinetics assay in presence of variable DHFA level | B | 6.3 | pKi | 500 | nM | Ki | Bioorg Med Chem (2009) 17: 7324-7336 [PMID:19748785] |
| dihydrofolate reductase/Dihydrofolate reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2363] [GtoPdb: 2603] [UniProtKB: Q920D2] | ||||||||
| ChEMBL | Inhibition of rat liver DHFR by enzyme kinetics assay in presence of variable DHFA level | B | 4.84 | pKi | 14300 | nM | Ki | Bioorg Med Chem (2009) 17: 7324-7336 [PMID:19748785] |
| ChEMBL | Inhibition of rat liver DHFR | B | 0.74 | pIC50 | 180000000 | nM | IC50 | J Med Chem (2007) 50: 3046-3053 [PMID:17552508] |
| ChEMBL | Inhibitory concentration against rat liver (RL) dihydrofolate reductases (DHFR) | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (1993) 36: 3437-3443 [PMID:8230134] |
| ChEMBL | Inhibition of Rat liver Dihydrofolate reductase(DHFR) | B | 4.47 | pIC50 | 34000 | nM | IC50 | J Med Chem (1988) 31: 122-129 [PMID:3121854] |
| Dihydrofolate reductase in Pneumocystis jirovecii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2057] [UniProtKB: Q9UUP5] | ||||||||
| ChEMBL | Inhibition of Pneumocystis jirovecii recombinant DHFR expressed in Escherichia coli Rosetta Gami B (DE3) competent cells using DHFA as substrate and NADPH | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem (2018) 26: 2640-2650 [PMID:29691153] |
| Dihydrofolate reductase in Salmonella enterica subsp. enterica serovar Typhi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4888] [UniProtKB: Q8Z9J9] | ||||||||
| ChEMBL | Inhibitory activity against Escherichia coli dihydrofolate reductase | B | 8.08 | pKi | 8.32 | nM | Ki | J Med Chem (1991) 34: 46-54 [PMID:1899453] |
| ChEMBL | Inhibitory activity against Escherichia coli dihydrofolate reductase | B | 8.08 | pKi | 8.32 | nM | Ki | J Med Chem (1991) 34: 46-54 [PMID:1899453] |
| Dihydrofolate reductase in Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296314] [UniProtKB: Q54801] | ||||||||
| ChEMBL | Inhibition of trimethoprim-resistant Streptococcus pneumoniae DHFR I100L mutant | B | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (2007) 50: 4374-4381 [PMID:17696333] |
| Dihydrofolate reductase in Lactococcus lactis subsp. lactis (strain IL1403) (Streptococcuslactis) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4012] [UniProtKB: Q59487] | ||||||||
| ChEMBL | In vitro inhibition of dihydrofolate reductase enzymes in Neisseria gonorrhoeae | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (1989) 32: 1949-1958 [PMID:2754716] |
| Dihydrofolate reductase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2576] [UniProtKB: P07807] | ||||||||
| ChEMBL | Inhibitory activity against Pneumocystis carinii dihydrofolate reductase. | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1996) 39: 1836-1845 [PMID:8627607] |
| Dihydrofolate reductase type 1 in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2627] [UniProtKB: P00382] | ||||||||
| ChEMBL | Inhibitory activity to dihydrofolate reductase in Escherichia coli | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1989) 32: 1927-1935 [PMID:2502632] |
| NH(3)-dependent NAD(+) synthetase in Bacillus subtilis (strain 168) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4615] [UniProtKB: P08164] | ||||||||
| ChEMBL | Inhibitory activity against Bacillus subtilis NAD synthetase | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 3371-3381 [PMID:12852767] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JB8 after 72 hrs by SYBR green assay | F | 4.15 | pIC50 | 70393 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum WE2 after 72 hrs by SYBR green assay | F | 4.21 | pIC50 | 61785 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum DAN after 72 hrs by SYBR green assay | F | 4.22 | pIC50 | 59746 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum KC2 after 72 hrs by SYBR green assay | F | 4.3 | pIC50 | 50695 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum AL2 after 72 hrs by SYBR green assay | F | 4.31 | pIC50 | 48456 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum DEV after 72 hrs by SYBR green assay | F | 4.32 | pIC50 | 48211 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JF6 after 72 hrs by SYBR green assay | F | 4.32 | pIC50 | 48189 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum KC5 after 72 hrs by SYBR green assay | F | 4.35 | pIC50 | 44582 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum XB3 after 72 hrs by SYBR green assay | F | 4.36 | pIC50 | 43831 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum KB8 after 72 hrs by SYBR green assay | F | 4.38 | pIC50 | 41742 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JB12 after 72 hrs by SYBR green assay | F | 4.4 | pIC50 | 40053 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 harboring polymorphic DHFR after 72 hrs by SYBR green assay | F | 4.4 | pIC50 | 40000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum XD8 after 72 hrs by SYBR green assay | F | 4.4 | pIC50 | 39806 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JC9 after 72 hrs by SYBR green assay | F | 4.4 | pIC50 | 39642 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum NF10 after 72 hrs by SYBR green assay | F | 4.4 | pIC50 | 39605 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 4.44 | pIC50 | 36531 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn, Asn51Ile and Cys59Arg triple mutant by [3H]hypoxanthine incorporation assay | F | 4.47 | pIC50 | 33655 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum WC4 after 72 hrs by SYBR green assay | F | 4.49 | pIC50 | 32669 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 harboring polymorphic DHFR after 72 hrs by SYBR green assay | F | 4.52 | pIC50 | 30000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D2 after 72 hrs by SYBR green assay | F | 4.53 | pIC50 | 29852 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Kenyan isolates by [3H]hypoxanthine incorporation assay | F | 4.53 | pIC50 | 29656 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum LC12 after 72 hrs by SYBR green assay | F | 4.62 | pIC50 | 24165 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| 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 | 5.03 | pIC50 | 9308.6 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | In vitro antiplasmodial activity (IC50) against Plasmodium falciparum wtTM4/8.2 | F | 5.17 | pIC50 | 6700 | nM | IC50 | J Med Chem (2002) 45: 1244-1252 [PMID:11881993] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 harboring polymorphic DHFR after 72 hrs by SYBR green assay | F | 5.39 | pIC50 | 4100 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum XG10 after 72 hrs by SYBR green assay | F | 5.48 | pIC50 | 3311 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 harboring polymorphic DHFR after 72 hrs by SYBR green assay | F | 5.55 | pIC50 | 2800 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum WF12 after 72 hrs by SYBR green assay | F | 5.58 | pIC50 | 2657 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against transgenic Plasmodium falciparum Dd2 pDT harboring polymorphic DHFR after 72 hrs by SYBR green assay | F | 5.59 | pIC50 | 2600 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum AUD after 72 hrs by SYBR green assay | F | 5.61 | pIC50 | 2481 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum NIC after 72 hrs by SYBR green assay | F | 5.64 | pIC50 | 2303 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum XF12 after 72 hrs by SYBR green assay | F | 5.64 | pIC50 | 2273 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum QF5 after 72 hrs by SYBR green assay | F | 5.67 | pIC50 | 2155 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum KA6 after 72 hrs by SYBR green assay | F | 5.68 | pIC50 | 2108 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JON after 72 hrs by SYBR green assay | F | 5.68 | pIC50 | 2071 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JC3 after 72 hrs by SYBR green assay | F | 5.69 | pIC50 | 2032 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JF11 after 72 hrs by SYBR green assay | F | 5.79 | pIC50 | 1640 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum JH6 after 72 hrs by SYBR green assay | F | 5.82 | pIC50 | 1503 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum KH7 after 72 hrs by SYBR green assay | F | 5.85 | pIC50 | 1412 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.9 | pIC50 | 1258.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.9 | pIC50 | 1258.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum LA10 after 72 hrs by SYBR green assay | F | 5.93 | pIC50 | 1183 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum TF1 after 72 hrs by SYBR green assay | F | 5.96 | pIC50 | 1096 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum XE7 after 72 hrs by SYBR green assay | F | 6.07 | pIC50 | 855 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antimalarial activity against pyrimethamine-sensitive Plasmodium falciparum 3D7 expressing wild type DHFR by [3H]hypoxanthine incorporation assay | F | 6.39 | pIC50 | 406.7 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3793-3798 [PMID:19528269] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCR3 infected in human erythrocytes by Giemsa staining analysis | F | 6.42 | pIC50 | 380.19 | nM | IC50 | Bioorg Med Chem (2019) 27: 3574-3586 [PMID:31272837] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.25 | pIC50 | 56800 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | B | 4.3 | pIC50 | 50680 | nM | IC50 | J Med Chem (2017) 60: 2685-2696 [PMID:28230985] |
| TAAR5/Trace amine-associated receptor 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784908] [GtoPdb: 170] [UniProtKB: Q5QD14] | ||||||||
| ChEMBL | Agonist activity at mouse TAAR5 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2017) 127: 781-792 [PMID:27823885] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
