pyrimethamine [Ligand Id: 4800] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL36 (Malacide, TCMDC-123831, GNF-PF-5586, Chloridin, Daraprim, Pyrimethamine, TCMDC-125860, WR-2978, NSC-3061, RP-4753)
  • Beta-hexosaminidase subunit alpha in Human [ChEMBL: CHEMBL1250415] [UniProtKB: P06865]
  • This target only has 0 pki data point
  • 0
1 CHEMBL36_lig_chart_1 Beta-hexosaminidase subunit alpha Human
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  • Beta-hexosaminidase subunit beta in Human [ChEMBL: CHEMBL5877] [UniProtKB: P07686]
  • This target only has 0 pki data point
  • 0
2 CHEMBL36_lig_chart_2 Beta-hexosaminidase subunit beta Human
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  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum V1/S [GtoPdb: 2981]
  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum K1 [GtoPdb: 2981]
  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum NF54 [GtoPdb: 2981]
  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase/Bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL4296323] [GtoPdb: 2981] [UniProtKB: Q8I1R6]
  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum 7G8 [GtoPdb: 2981]
  • Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum D6 [GtoPdb: 2981]
  • This target only has 1 pki data point
  • 0
3 CHEMBL36_lig_chart_3 Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase Plasmodium falciparum V1/SPlasmodium falciparum K1Plasmodium falciparum NF54Plasmodium falciparum 3D7Plasmodium falciparum 7G8Plasmodium falciparum D6
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  • Dihydrofolate reductase in Escherichia coli [ChEMBL: CHEMBL5441] [UniProtKB: B0BL08]
  • Dihydrofolate reductase in Pneumocystis carinii [ChEMBL: CHEMBL1926] [UniProtKB: P16184]
  • Dihydrofolate reductase in Candida albicans [ChEMBL: CHEMBL2329] [UniProtKB: P22906]
  • Dihydrofolate reductase in Toxoplasma gondii [ChEMBL: CHEMBL2425] [UniProtKB: Q07422]
  • Dihydrofolate reductase in Plasmodium falciparum K1 [ChEMBL: CHEMBL1939] [UniProtKB: P13922]
  • dihydrofolate reductase/Dihydrofolate reductase in Human [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374]
  • Dihydrofolate reductase in Bovine [ChEMBL: CHEMBL1075051] [UniProtKB: P00376]
  • dihydrofolate reductase/Dihydrofolate reductase in Rat [ChEMBL: CHEMBL2363] [GtoPdb: 2603] [UniProtKB: Q920D2]
  • 0
4 CHEMBL36_lig_chart_4 Dihydrofolate reductase Escherichia coliPneumocystis cariniiCandida albicansToxoplasma gondiiPlasmodium falciparum K1HumanBovineRat
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  • Multidrug and toxin extrusion in Human [GtoPdb: 1216] [UniProtKB: Q96FL8]
  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Mouse [ChEMBL: CHEMBL3091264] [GtoPdb: 1216] [UniProtKB: Q8K0H1]
  • 6.84
5 CHEMBL36_lig_chart_5 Multidrug and toxin extrusion HumanMouse
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  • Plasmodium berghei [ChEMBL: CHEMBL612653]
  • This target only has 0 pki data point
  • 0
6 CHEMBL36_lig_chart_6 Plasmodium berghei Plasmodium berghei
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  • Plasmodium cynomolgi [ChEMBL: CHEMBL613883]
  • This target only has 0 pki data point
  • 0
7 CHEMBL36_lig_chart_7 Plasmodium cynomolgi Plasmodium cynomolgi
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
8 CHEMBL36_lig_chart_8 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium falciparum 3D7 [ChEMBL: CHEMBL2366922]
  • This target only has 0 pki data point
  • 0
9 CHEMBL36_lig_chart_9 Plasmodium falciparum 3D7 Plasmodium falciparum 3D7
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  • Plasmodium falciparum D6 [ChEMBL: CHEMBL2367107]
  • This target only has 0 pki data point
  • 0
10 CHEMBL36_lig_chart_10 Plasmodium falciparum D6 Plasmodium falciparum D6
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
  • This target only has 0 pki data point
  • 0
11 CHEMBL36_lig_chart_11 Plasmodium falciparum (isolate K1 / Thailand) Plasmodium falciparum K1
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  • Plasmodium falciparum NF54 [ChEMBL: CHEMBL2367131]
  • This target only has 0 pki data point
  • 0
12 CHEMBL36_lig_chart_12 Plasmodium falciparum NF54 Plasmodium falciparum NF54
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  • Plasmodium yoelii [ChEMBL: CHEMBL612889]
  • This target only has 0 pki data point
  • 0
13 CHEMBL36_lig_chart_13 Plasmodium yoelii Plasmodium yoelii
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  • Pteridine reductase 1 in Leishmania major [ChEMBL: CHEMBL6194] [UniProtKB: Q01782]
  • This target only has 0 pki data point
  • 0
14 CHEMBL36_lig_chart_14 Pteridine reductase 1 Leishmania major
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
  • This target only has 1 pki data point
  • 5.44
15 CHEMBL36_lig_chart_15 Solute carrier family 22 member 1 HumanMouse
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  • TAAR5/Trace amine-associated receptor 5 in Mouse [ChEMBL: CHEMBL3784908] [GtoPdb: 170] [UniProtKB: Q5QD14]
  • This target only has 0 pki data point
  • 0
16 CHEMBL36_lig_chart_16 Trace amine-associated receptor 5 Mouse
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  • MATE2 in Mouse [GtoPdb: 1217] [UniProtKB: Q3V050]
  • This target only has 1 pki data point
  • 6.3
17 CHEMBL36_lig_chart_17 MATE2 Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Beta-hexosaminidase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250415] [UniProtKB: P06865]
ChEMBL Inhibition of HexA alpha G269S mutant in ATSD patient fibroblasts using MUGS substrate incubated for 1 to 2 hrs at pH 4.5 by spectrofluorometry B 5.07 pIC50 8500 nM IC50 J. Med. Chem. (2015) 58: 4483-4493 [PMID:25984755]
Beta-hexosaminidase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5877] [UniProtKB: P07686]
ChEMBL Inhibition of human placental HexB using MUGS substrate incubated for 1 to 2 hrs at pH 4.5 by spectrofluorometry B 5.04 pIC50 9100 nM IC50 J. Med. Chem. (2015) 58: 4483-4493 [PMID:25984755]
ChEMBL Inhibition of human placental HexB using MUGS substrate incubated for 1 to 2 hrs at pH 7.0 by spectrofluorometry B 5.35 pIC50 4500 nM IC50 J. Med. Chem. (2015) 58: 4483-4493 [PMID:25984755]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum V1/S [GtoPdb: 2981]
GtoPdb Parasite growth inhibition assay - 4 pIC50 >100000 nM IC50 Proc Natl Acad Sci USA (2012) 109: 16823-8 [PMID:23035243]
GtoPdb Parasite growth inhibition assay - 5 pIC50 >10000 nM IC50 PLoS Med (2012) 9: e1001169 [PMID:22363211]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum K1 [GtoPdb: 2981]
GtoPdb Parasite growth inhibition assay - 5 pIC50 >10000 nM IC50 PLoS Med (2012) 9: e1001169 [PMID:22363211]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum NF54 [GtoPdb: 2981]
GtoPdb Parasite growth inhibition assay - 7.77 pIC50 17 nM IC50 PLoS Med (2012) 9: e1001169 [PMID:22363211]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase/Bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296323] [GtoPdb: 2981] [UniProtKB: Q8I1R6]
ChEMBL Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay B 9.07 pKi 0.85 nM Ki Antimicrob. Agents Chemother. (2007) 51: 4356-4360 [PMID:17875995]
ChEMBL Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3) B 5.61 pIC50 2480 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 4356-4360 [PMID:17875995]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum 7G8 [GtoPdb: 2981]
GtoPdb Parasite growth inhibition assay - 5.17 pIC50 6688.7 nM IC50 PLoS Med (2012) 9: e1001169 [PMID:22363211]
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum D6 [GtoPdb: 2981]
GtoPdb Parasite growth inhibition assay - 8.34 pIC50 4.6 nM IC50 PLoS Med (2012) 9: e1001169 [PMID:22363211]
Dihydrofolate reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5441] [UniProtKB: B0BL08]
ChEMBL Thermodynamic dissociation constant of compound for mutant T46N Escherichia coli dihydrofolate reductase B 7.8 pKd 16 nM Kd J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Thermodynamic dissociation constant of compound for wild type Escherichia coli dihydrofolate reductase B 7.89 pKd 13 nM Kd J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Thermodynamic dissociation constant of compound for mutant T46S Escherichia coli dihydrofolate reductase B 8.82 pKd 1.5 nM Kd J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Thermodynamic dissociation constant of compound for mutant T46A Escherichia coli dihydrofolate reductase B 8.85 pKd 1.4 nM Kd J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Inhibition constant against binding of Escherichia coli dihydrofolate reductase B 6.55 pKi 281.84 nM Ki J. Med. Chem. (1988) 31: 1396-1406 [PMID:3290487]
ChEMBL Inhibitor constant of compound for mutant T46N Escherichia coli dihydrofolate reductase B 7.7 pKi 20 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Inhibitor constant of compound for wild type Escherichia coli dihydrofolate reductase B 8 pKi 10 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Inhibitor constant of compound for mutant T46S Escherichia coli dihydrofolate reductase B 8.28 pKi 5.2 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Inhibitor constant of compound for mutant T46A Escherichia coli dihydrofolate reductase B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Inhibition of Escherichia coli DHFR B 5.18 pIC50 6600 nM IC50 Bioorg. Med. Chem. (2012) 20: 4217-4225 [PMID:22739090]
ChEMBL Inhibition of Escherichia coli dihydrofolate reductase B 5.7 pIC50 2000 nM IC50 J. Med. Chem. (2008) 51: 4589-4600 [PMID:18605720]
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 8.01 pKi 9.7 nM Ki J. Med. Chem. (1995) 38: 4739-4759 [PMID:7490723]
ChEMBL Inhibition of Dihydrofolate reductase of Pneumocystis carinii B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1994) 37: 4522-4528 [PMID:7799402]
ChEMBL Inhibitory activity against Pneumocystis carinii Dihydrofolate reductase B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1995) 38: 745-752 [PMID:7877140]
ChEMBL Inhibition of Pneumocystis carinii Dihydrofolate Reductase B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1997) 40: 3694-3699 [PMID:9357537]
ChEMBL In vitro inhibitory concentration against Pneumocystis carinii dihydrofolate reductase B 5.44 pIC50 3650 nM IC50 J. Med. Chem. (1997) 40: 1886-1893 [PMID:9191966]
ChEMBL Inhibitory activity against Pneumocystis carinii dihydrofolate reductase B 5.44 pIC50 3650 nM IC50 J. Med. Chem. (1996) 39: 1271-1280 [PMID:8632434]
ChEMBL Inhibitory activity against dihydrofolate reductase in Pneumocystis carinii at 37 centigrade. B 5.55 pIC50 2800 nM IC50 J. Med. Chem. (1995) 38: 4739-4759 [PMID:7490723]
ChEMBL Compound was tested for inhibition activity against pneumocystis carinii (Pneumocystis carinii) Dihydrofolate reductase B 5.62 pIC50 2400 nM IC50 J. Med. Chem. (1998) 41: 913-918 [PMID:9526565]
ChEMBL Inhibition of Pneumocystis carinii DHFR B 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2013) 56: 4422-4441 [PMID:23627352]
Dihydrofolate reductase in Candida albicans (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2329] [UniProtKB: P22906]
ChEMBL Inhibition of dihydrofolate reductase in Candida albicans (in vitro). B 5.3 pIC50 5000 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 Compound was tested for inhibition activity against Toxoplasma gondii (Toxoplasma gondii) Dihydrofolate reductase B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1998) 41: 913-918 [PMID:9526565]
ChEMBL Inhibitory activity against Toxoplasma gondii dihydrofolate reductase B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1996) 39: 1271-1280 [PMID:8632434]
ChEMBL Inhibitory activity against Toxoplasma gondii Dihydrofolate reductase B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1995) 38: 745-752 [PMID:7877140]
ChEMBL The ability to inhibit Toxoplasma gondii Dihydrofolate reductase was tested B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1999) 42: 1007-1017 [PMID:10090784]
ChEMBL Inhibitory activity against dihydrofolate reductase DHFR in Toxoplasma gondii. B 6.41 pIC50 390 nM IC50 J. Med. Chem. (2001) 44: 2555-2564 [PMID:11472209]
ChEMBL Inhibition of Toxoplasma gondii Dihydrofolate Reductase B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1997) 40: 3694-3699 [PMID:9357537]
ChEMBL Inhibitory concentration against Toxoplasma gondii dihydrofolate reductase B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1997) 40: 1886-1893 [PMID:9191966]
ChEMBL Inhibition of Dihydrofolate reductase of Toxoplasma gondii B 6.41 pIC50 390 nM IC50 J. Med. Chem. (1994) 37: 4522-4528 [PMID:7799402]
ChEMBL Inhibition of Toxoplasma gondii TS-DHFR expressed in Escherichia coli BL21 preincubated for 15 mins followed by addition of DHF as substrate and NADPH measured after 60 mins by resazurin/diaphorase coupled assay B 6.64 pIC50 230 nM IC50 ACS Med Chem Lett (2016) 7: 1124-1129 [PMID:27994750]
ChEMBL Inhibition of Toxoplasma gondii DHFR B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. (2012) 20: 4217-4225 [PMID:22739090]
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 6.86 pIC50 139 nM IC50 J Med Chem (2019) 62: 1562-1576 [PMID:30624926]
ChEMBL Inhibition of Toxoplasma gondii dihydrofolate reductase B 7.1 pIC50 80 nM IC50 J. Med. Chem. (2008) 51: 4589-4600 [PMID:18605720]
Dihydrofolate reductase in Plasmodium falciparum K1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1939] [UniProtKB: P13922]
ChEMBL Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with quadruple (N51I + C59R + S108N + I164L) mutations B 6.07 pKi 860 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum B 6.41 pKi 385 nM Ki J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with triple (C59R + S108N + I164L) mutations B 6.42 pKi 380 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum B 6.95 pKi 112 nM Ki J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Binding affinity was evaluated as inhibition of mutant (C59R + S108N) Plasmodium falciparum DHFR-TS. B 7.14 pKi 71.7 nM Ki J. Med. Chem. (1998) 41: 1367-1370 [PMID:9554869]
ChEMBL Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum B 7.17 pKi 67.1 nM Ki J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) B 7.27 pKi 53.9 nM Ki J. Med. Chem. (2002) 45: 1244-1252 [PMID:11881993]
ChEMBL Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) B 7.54 pKi 28.6 nM Ki J. Med. Chem. (2002) 45: 1244-1252 [PMID:11881993]
ChEMBL Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single A16V mutation B 8.22 pKi 6 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with double (A16V + S108T) mutations B 8.44 pKi 3.6 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Inhibitor constant of compound for mutant S108 N Plasmodium falciparum in dihydrofolate reductase B 8.7 pKi 2 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL Binding affinity was evaluated as inhibition of recombinant wild type (WT) Plasmodium falciparum DHFR-TS. B 8.82 pKi 1.5 nM Ki J. Med. Chem. (1998) 41: 1367-1370 [PMID:9554869]
ChEMBL Inhibition constant against wild-type PfDHFR (Plasmodium falciparum dihydrofolate reductase) B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single S108T mutation B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2003) 46: 2834-2845 [PMID:12825927]
ChEMBL Inhibition constant against Plasmodium falciparum dihydrofolate reductase B 9.06 pKi 0.87 nM Ki J. Med. Chem. (2004) 47: 4258-4267 [PMID:15293997]
ChEMBL Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum. B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Inhibition of the wild-type dihydrofolate reductase (DHFR) B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2002) 45: 1244-1252 [PMID:11881993]
ChEMBL Inhibitor constant of compound for Plasmodium falciparum dihydrofolate reductase B 9.72 pKi 0.19 nM Ki J. Med. Chem. (1992) 35: 2912-2915 [PMID:1495020]
ChEMBL In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase CN51I/C59R/S108N/I164L (V1/S) mutant F 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase N51I/C59R/S108N (W2) F 4.13 pIC50 73500 nM IC50 J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase C59R+S108N/I164L (Csl-2) mutant F 4.38 pIC50 41700 nM IC50 J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Antiplasmodial activity IC50 against Plasmodium falciparum K1CB1 DHFR double-mutant (C59R/S10) F 4.51 pIC50 30900 nM IC50 J. Med. Chem. (2002) 45: 1244-1252 [PMID:11881993]
ChEMBL In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase wild type (TM4/8.2) F 7.1 pIC50 80 nM IC50 J. Med. Chem. (2004) 47: 673-680 [PMID:14736247]
ChEMBL Inhibition of Plasmodium falciparum DHFR B 7.1 pIC50 80 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 4366-4370 [PMID:16750361]
ChEMBL Inhibition of Plasmodium falciparum DHFR B 7.24 pIC50 58 nM IC50 Bioorg Med Chem (2017) 25: 6467-6478 [PMID:29111368]
ChEMBL Inhibition of Plasmodium falciparum DHFR using DHF as substrate preincubated for 15 mins followed DHF addition measured after 15 mins by spectrophotometric method B 7.59 pIC50 25.5 nM IC50 Bioorg Med Chem (2017) 25: 6467-6478 [PMID:29111368]
dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374]
ChEMBL Inhibition of human DHFR using dihydrofolate as substrate after 180 secs by spectrophotometric analysis B 6.33 pKi 470 nM Ki Eur J Med Chem (2017) 135: 467-478 [PMID:28477572]
ChEMBL Inhibition of recombinant Dihydrofolate reductase from Leishmania major. B 6.6 pKi 250 nM Ki J. Med. Chem. (1999) 42: 4300-4312 [PMID:10543874]
ChEMBL Inhibition of recombinant Dihydrofolate reductase from humans. B 6.92 pKi 120 nM Ki J. Med. Chem. (1999) 42: 4300-4312 [PMID:10543874]
ChEMBL Inhibition of recombinant Dihydrofolate reductase from Trypanosoma cruzi. B 7.01 pKi 98 nM Ki J. Med. Chem. (1999) 42: 4300-4312 [PMID:10543874]
ChEMBL Binding affinity to human recombinant DHFR expressed in Escherichia coli BL21(DE3) by competitive binding assay B 7.51 pKi 30.8 nM Ki Antimicrob. Agents Chemother. (2010) 54: 2603-2610 [PMID:20350951]
ChEMBL Inhibition of recombinant Dihydrofolate reductase from humans. B 7.96 pKi 11 nM Ki J. Med. Chem. (1999) 42: 4300-4312 [PMID:10543874]
ChEMBL Cytotoxicity by selective inhibition against human dihydrofolate reductase (DHFR). B 8.1 pKi 8 nM Ki J. Med. Chem. (2002) 45: 1244-1252 [PMID:11881993]
ChEMBL Inhibition of human dihydrofolate reductase B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (2008) 51: 4589-4600 [PMID:18605720]
ChEMBL Inhibition of human DHFR B 5.22 pIC50 6000 nM IC50 Bioorg. Med. Chem. (2012) 20: 4217-4225 [PMID:22739090]
ChEMBL In vitro inhibition of human dihydrofolate reductase B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (1995) 38: 3608-3616 [PMID:7658448]
ChEMBL Inhibition of human recombinant DHFR B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2013) 56: 4422-4441 [PMID:23627352]
Dihydrofolate reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075051] [UniProtKB: P00376]
ChEMBL Inhibition of bovine liver DHFR B 7 pIC50 100.7 nM IC50 Bioorg Med Chem (2017) 25: 5396-5406 [PMID:28789907]
ChEMBL