PYRIMETHAMINE

/static/temp/default.svg Search structure
Trade Names
Synonyms
Status
Molecule Category Free-form
ATC P01BD01
UNII Z3614QOX8W
EPA CompTox DTXSID9021217

Structure

InChI Key WKSAUQYGYAYLPV-UHFFFAOYSA-N
Smiles CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1
InChI
InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)

Physicochemical Descriptors

Property Name Value
Molecular Formula C12H13ClN4
Molecular Weight 248.72
AlogP 2.52
Hydrogen Bond Acceptor 4.0
Hydrogen Bond Donor 2.0
Number of Rotational Bond 2.0
Polar Surface Area 77.82
Molecular species NEUTRAL
Aromatic Rings 2.0
Heavy Atoms 17.0

Bioactivity

Mechanism of Action Action Reference
Dihydrofolate reductase inhibitor INHIBITOR DailyMed Wikipedia
Targets EC50(nM) IC50(nM) Kd(nM) Ki(nM) Inhibition(%)
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C9
- - - 51500 -
Enzyme Hydrolase
- 3100-17000 - - -
Enzyme Oxidoreductase
- 80-390 1-16 0-860 -
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC21/SLCO family of organic anion transporting polypeptides
- - - - 107
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC22 family of organic cation and anion transporters
- 13570 - 3600 -
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC47 family of multidrug and toxin extrusion transporters
- - - 145 -
Unclassified protein
- 2480 - 1 -
Assay Description Organism Bioactivity Reference
Binding affinity was reported with purified recombinant Pneumocystis carinii Dihydrofolate reductase Pneumocystis carinii 9.7 nM
Inhibition of Toxoplasma gondii Dihydrofolate Reductase Toxoplasma gondii 390.0 nM
Compound was tested for inhibition activity against Toxoplasma gondii (Toxoplasma gondii) Dihydrofolate reductase Toxoplasma gondii 390.0 nM
Inhibitory concentration against Toxoplasma gondii dihydrofolate reductase Toxoplasma gondii 390.0 nM
Inhibition of Dihydrofolate reductase of Toxoplasma gondii Toxoplasma gondii 390.0 nM
Inhibitory activity against dihydrofolate reductase DHFR in Toxoplasma gondii. Toxoplasma gondii 390.0 nM
Inhibitory activity against Toxoplasma gondii Dihydrofolate reductase Toxoplasma gondii 390.0 nM
Inhibitory activity against Toxoplasma gondii dihydrofolate reductase Toxoplasma gondii 390.0 nM
The ability to inhibit Toxoplasma gondii Dihydrofolate reductase was tested Toxoplasma gondii 390.0 nM
Inhibition of recombinant Dihydrofolate reductase from humans. Trypanosoma brucei 11.0 nM
Inhibition of recombinant Dihydrofolate reductase from Trypanosoma cruzi. Trypanosoma cruzi 98.0 nM
Cytotoxicity by selective inhibition against human dihydrofolate reductase (DHFR). None 8.0 nM
Inhibition of recombinant Dihydrofolate reductase from humans. None 120.0 nM
Thermodynamic dissociation constant of compound for mutant T46A Escherichia coli dihydrofolate reductase Escherichia coli 1.4 nM
Thermodynamic dissociation constant of compound for mutant T46N Escherichia coli dihydrofolate reductase Escherichia coli 16.0 nM
Thermodynamic dissociation constant of compound for mutant T46S Escherichia coli dihydrofolate reductase Escherichia coli 1.5 nM
Thermodynamic dissociation constant of compound for wild type Escherichia coli dihydrofolate reductase Escherichia coli 13.0 nM
Inhibitor constant of compound for mutant T46A Escherichia coli dihydrofolate reductase Escherichia coli 1.2 nM
Inhibitor constant of compound for mutant T46N Escherichia coli dihydrofolate reductase Escherichia coli 20.0 nM
Inhibitor constant of compound for mutant T46S Escherichia coli dihydrofolate reductase Escherichia coli 5.2 nM
Inhibitor constant of compound for wild type Escherichia coli dihydrofolate reductase Escherichia coli 10.0 nM
Inhibition constant against binding of Escherichia coli dihydrofolate reductase Escherichia coli 281.84 nM
Inhibition of recombinant Dihydrofolate reductase from Leishmania major. Leishmania major 250.0 nM
Inhibitor constant of compound for mutant S108 N Plasmodium falciparum in dihydrofolate reductase Plasmodium falciparum 2.0 nM
Inhibitor constant of compound for Plasmodium falciparum dihydrofolate reductase Plasmodium falciparum 0.19 nM
Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum Plasmodium falciparum 112.0 nM
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum Plasmodium falciparum 67.1 nM
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum Plasmodium falciparum 385.0 nM
Inhibition constant against wild-type PfDHFR (Plasmodium falciparum dihydrofolate reductase) Plasmodium falciparum 1.5 nM
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) Plasmodium falciparum 53.9 nM
Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) Plasmodium falciparum 28.6 nM
Inhibition of the wild-type dihydrofolate reductase (DHFR) Plasmodium falciparum 0.6 nM
Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with double (A16V + S108T) mutations Plasmodium falciparum 3.6 nM
Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with quadruple (N51I + C59R + S108N + I164L) mutations Plasmodium falciparum 860.0 nM
Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single A16V mutation Plasmodium falciparum 6.0 nM
Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single S108T mutation Plasmodium falciparum 1.4 nM
Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with triple (C59R + S108N + I164L) mutations Plasmodium falciparum 380.0 nM
The ability to inhibit [3H]- uracil incorporation by Toxoplasma gondii in cultures of HEL cells was tested Homo sapiens 670.0 nM
In vitro antiplasmodial activity (IC50) against Plasmodium falciparum wtTM4/8.2 Plasmodium falciparum 80.0 nM
In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase wild type (TM4/8.2) Plasmodium falciparum 80.0 nM
In vitro inhibition of Plasmodium falciparum HB3 (S108N) culture Plasmodium falciparum 1.2 nM
In vitro inhibition of Plasmodium falciparum K1 (S108N + C59R) culture Plasmodium falciparum 10.2 nM
Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes by semiautomated micro dilution Plasmodium falciparum 30.0 nM
Antimalarial activity against Plasmodium falciparum 3D7 in erythrocytes Plasmodium falciparum 3.0 nM
Inhibition of Toxoplasma gondii cell growth Toxoplasma gondii 400.0 nM
Binding affinity was evaluated as inhibition of mutant (C59R + S108N) Plasmodium falciparum DHFR-TS. Plasmodium falciparum 71.7 nM
Binding affinity was evaluated as inhibition of recombinant wild type (WT) Plasmodium falciparum DHFR-TS. Plasmodium falciparum 1.5 nM
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum. Plasmodium falciparum 0.6 nM
Inhibition constant against Plasmodium falciparum dihydrofolate reductase Plasmodium falciparum 0.87 nM
Inhibitory concentration against cycloguanil sensitive Plasmodium falciparum FJB-D4 Plasmodium falciparum 5.0 nM
Inhibitory concentration against cycloguanil sensitive Plasmodium falciparum FJB-D9 Plasmodium falciparum 1.6 nM
In vitro antimalarial activity for DHFR wild-type, chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 Plasmodium falciparum 0.13 ug.mL-1
In vitro antimalarial activity for DHFR wild-type, chloroquine and pyrimethamine-sensitive Plasmodium falciparum D6 Plasmodium falciparum 0.0012 ug.mL-1
Inhibition of Plasmodium falciparum DHFR Plasmodium falciparum 80.0 nM
Growth inhibition of Plasmodium falciparum 3D7 ring stage in infected erythrocytes after 72 hrs in DAPI fluorimetry Plasmodium falciparum 10.01 nM
Growth inhibition of Plasmodium falciparum HB3 ring stage in infected erythrocytes after 72 hrs in DAPI fluorimetry Plasmodium falciparum 49.88 nM
Growth inhibition of Plasmodium falciparum Dd2 ring stage infected erythrocytes after 72 hrs by DAPI fluorimetry Plasmodium falciparum 44.1 nM
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay Plasmodium falciparum 0.0005 ug.mL-1
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay Plasmodium falciparum 0.0083 ug.mL-1
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay Plasmodium falciparum 0.0004 ug.mL-1
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay Plasmodium falciparum 0.0376 ug.mL-1
Antimalarial activity against Plasmodium falciparum D6 as reduced [3H]hypoxanthine uptake after 72 hrs Plasmodium falciparum 0.0001 ug.mL-1
Antimalarial activity against Plasmodium falciparum W2 as reduced [3H]hypoxanthine uptake after 72 hrs Plasmodium falciparum 0.0119 ug.mL-1
Inhibition of Toxoplasma gondii dihydrofolate reductase Toxoplasma gondii 80.0 nM
Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Toxoplasma gondii 210.0 nM
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-1 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Toxoplasma gondii 290.0 nM
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-6 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Toxoplasma gondii 270.0 nM
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii STL500-10A infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Toxoplasma gondii 240.0 nM
Inhibition of pyrimethamine-resistant form-3 Plasmodium falciparum N51I, C59R, S108N, I164L, I150V, N182I, N201D mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 1.07 nM
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 Plasmodium falciparum 0.85 nM
Inhibition of pyrimethamine-resistant form-1 Plasmodium falciparum N51I, C59R, S108N, I164L, D187A mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 1.24 nM
Inhibition of WR99210-resistant form-3 Plasmodium falciparum N51I, C59R, N108T, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 15.5 nM
Inhibition of WR99210-resistant form-1 Plasmodium falciparum I51N, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 3.57 nM
Inhibition of Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 1.9 nM
Inhibition of Plasmodium falciparum DHFR-TS QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 2.1 nM
Inhibition of Plasmodium falciparum DHFR-TS QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) Plasmodium falciparum 170.0 nM
Inhibition of Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) Plasmodium falciparum 420.0 nM
Inhibition of WR99210-resistant form-1 Plasmodium falciparum I51N, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) Plasmodium falciparum 90.0 nM
Inhibition of WR99210-resistant form-2 Plasmodium falciparum N51I, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) Plasmodium falciparum 10.0 nM
Inhibition of pyrimethamine-resistant form-1 Plasmodium falciparum N51I, C59R, S108N, I164L, D187A mutant expressed in Escherichia coli BL21(DE3) Plasmodium falciparum 870.0 nM
Inhibition of WR99210-resistant form-2 Plasmodium falciparum N51I, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay Plasmodium falciparum 7.26 nM
Antiplasmodial activity against Plasmodium falciparum Plasmodium falciparum 4.083 ug.mL-1
Antiplasmodial activity against Plasmodium vivax Plasmodium vivax 0.008 ug.mL-1
Antimalarial activity as inhibition of schizont maturation against Plasmodium malariae Thai after 40 - 70 hrs Plasmodium malariae 0.00224 ug.mL-1
GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM Plasmodium falciparum 94.0 % GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM Plasmodium falciparum 93.0 %
GSK_TCMDC: Inhibition of Plasmodium falciparum Dd2 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM Plasmodium falciparum 0.0 % GSK_TCMDC: Inhibition of Plasmodium falciparum Dd2 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM Plasmodium falciparum 0.0 %
GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 LDH activity, using an LDH reporter assay. Test compounds present at 2uM Plasmodium falciparum 0.0 % GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 LDH activity, using an LDH reporter assay. Test compounds present at 2uM Plasmodium falciparum 5.0 %
GSK_TCMDC: Percent inhibition of human HepG2 cell line. Test compounds present at 10uM. Homo sapiens 71.0 % GSK_TCMDC: Percent inhibition of human HepG2 cell line. Test compounds present at 10uM. Homo sapiens 66.0 %
NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay Plasmodium falciparum 31.9 nM
NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay Plasmodium falciparum 14.56 nM
Antimicrobial activity against Toxoplasma gondii infected in HEL cells assessed as inhibition of parasite growth by [3H]uracil incorporation assay Toxoplasma gondii 700.0 nM
Antimicrobial activity against Toxoplasma gondii Toxoplasma gondii 0.0 nM
Antimicrobial activity against Pneumocystis carinii Pneumocystis carinii 0.0 nM
Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum clinical isolate harboring S108N, N51I mutation in DHFR assessed as decrease in parasitaemia Plasmodium falciparum 371.0 nM
Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum clinical isolate harboring S108N, C59R mutation in DHFR assessed as decrease in parasitaemia Plasmodium falciparum 371.0 nM
Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum clinical isolate harboring S108N, N51I, C59R mutation in DHFR assessed as decrease in parasitaemia Plasmodium falciparum 778.28 nM
Binding affinity to wild type Plasmodium falciparum DHFR by competitive binding assay Plasmodium falciparum 0.59 nM
Binding affinity to recombinant Plasmodium falciparum V1/S DHFR S108N, N51I, C59R, I164L mutant by competitive binding assay Plasmodium falciparum 385.0 nM
Binding affinity to human recombinant DHFR expressed in Escherichia coli BL21(DE3) by competitive binding assay Homo sapiens 30.8 nM
Antimicrobial activity against Toxoplasma gondii ENT harboring DHPS Ex2, E474D/Ex3, 156 sil Leu/Ex4, R560K/Ex5, 580 sil Gly/A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.34 ug.mL-1
Antimicrobial activity against Toxoplasma gondii B1 harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.35 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate RMS-1995-ABE harboring DHPS Ex5, A587V mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.17 ug.mL-1
Antimicrobial activity against Toxoplasma gondii ME49 infected in human MRC-5 cells infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.09 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate TRS-2004-REV infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.18 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate TOU-1998-TRI infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.15 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate RMS-2005-HAG infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.11 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate GRE-1995-MAE infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.11 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate PSP-2005-MUP infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.14 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate GRE-1998-TRA infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.39 ug.mL-1
Antimicrobial activity against Toxoplasma gondii NED infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.19 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate RMS-1994-LEF harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 204 sil Ala mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.07 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate RMS-2003-DJO infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.09 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate RMS-2001-MAU infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.12 ug.mL-1
Antimicrobial activity against Toxoplasma gondii isolate GUY-2003-MEL harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex2, 145 sil Val mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii 0.25 ug.mL-1
Antimicrobial activity against Toxoplasma gondii RH harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Toxoplasma gondii RH 0.1 ug.mL-1
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhibitors of of 5'UTR Stem-Loop Driven Alpha-Synuclein mRNA Translation in H4 Neuroglioblastoma Cells. (Class of assay: confirmatory) [Related pubchem assays: 1827 (Project Summary), 1813 (Primary HTS)] None 200.0 nM
Antileishmanial activity against Leishmania mexicana MHOM/BZ/84/BEL46 assessed as growth at 50 ug/ml by Alamar blue assay Leishmania mexicana 102.5 %
Antileishmanial activity against Leishmania major MHOM/SU/73/5-ASKH assessed as growth at 50 ug/ml by Alamar blue assay Leishmania major 68.0 %
Antimalarial activity against pyrimethamine-sensitive Plasmodium falciparum 3D7 expressing wild type DHFR by [3H]hypoxanthine incorporation assay Plasmodium falciparum 3.9 nM
Antimalarial activity against Plasmodium falciparum Kenyan isolates by [3H]hypoxanthine incorporation assay Plasmodium falciparum 733.26 nM
Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn and Cys59Arg or Ser108Asn and Asn51Ile double mutant by [3H]hypoxanthine incorporation assay Plasmodium falciparum 371.0 nM
Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn, Asn51Ile and Cys59Arg triple mutant by [3H]hypoxanthine incorporation assay Plasmodium falciparum 778.28 nM
Inhibition of Babesia gibsoni Dihydrofolate reductase-thymidylate synthase expressed in Escherichia coli BL21 Babesia gibsoni 50.0 nM
Antimalarial activity against Plasmodium falciparum D6 infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 0.028 nM
Antimalarial activity against Plasmodium falciparum TM91c235 harboring DHFR F57L, S58R, T61M, S117T mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 142.61 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 0.055 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 2.5 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 3.66 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 6.26 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R, T61M and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 2.81 nM
Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L, S58R, T61M, S117T mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs Plasmodium falciparum 467.34 nM
Antimalarial activity against Plasmodium falciparum 3D7 infected in human A positive erythrocytes by [3H]hypoxanthine uptake assay in presence of serum in medium Plasmodium falciparum 23.0 nM
NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration Plasmodium yoelii 2.152 nM
Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as decrease in parasitemia after 72 hrs Plasmodium falciparum 29.0 nM
Antimalarial activity against Plasmodium falciparum NF54 Plasmodium falciparum 19.0 nM
Antimalarial activity against Plasmodium falciparum FC27 Plasmodium falciparum FC27/Papua New Guinea 60.0 nM
Antimalarial activity against Plasmodium falciparum FCR3 Plasmodium falciparum FCR-3/Gambia 12.0 nM
Antimalarial activity against Plasmodium falciparum Mad20 Plasmodium falciparum Mad20/Papua New Guinea 60.0 nM
Inhibition of Plasmodium falciparum DHFR assessed as oxidation of NADPH to NADP+ at 10 uM after 15 mins spectrophotometric assay Plasmodium falciparum 98.9 %
Inhibition of Plasmodium falciparum DHFR assessed as oxidation of NADPH to NADP+ after 15 mins spectrophotometric assay Plasmodium falciparum 20.0 nM
Antitoxoplasmic activity against Toxoplasma gondii PRU tachyzoites infected in human HFF cells assessed as beta-galactosidase activity after 72 hrs by colorimetric assay Toxoplasma gondii PRU 800.0 nM
Antimicrobial activity against tachyzoites of Toxoplasma gondii expressing PRU-beta-Gal gene infected in HFF after 72 hrs by colorimetric microtiter assay Toxoplasma gondii 800.0 nM
Inhibition of Toxoplasma gondii DHFR Toxoplasma gondii 200.0 nM
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by parasitic LDH assay Plasmodium falciparum 10.0 nM
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells Plasmodium berghei 4.7 nM
OSM: Inhibition of Plasmodium falciparum 3D7 growth. IC50 values determined from 21 point dose response curves. Avery Group Griffith. Plasmodium falciparum 3D7 8.95 nM
OSM: Inhibition of Plasmodium falciparum 3D7 growth using a SYBR green I fluorescence based assay. GSK Tres Cantos. Plasmodium falciparum 3D7 33.2 nM
Antiplasmodial activity against Plasmodium falciparum 3D7A assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting Plasmodium falciparum 20.0 nM
Antimalarial activity against chloroquine-susceptible Plasmodium falciparum D10 asexual erythrocyte forms after 48 hrs by parasite LDH assay Plasmodium falciparum D10 70.0 nM
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Chlorocebus sabaeus 62.5 ug.mL-1
SANGER: Inhibition of human ES1 cell growth in a cell viability assay. Homo sapiens 122.9 nM
SANGER: Inhibition of human ES8 cell growth in a cell viability assay. Homo sapiens 896.67 nM
SANGER: Inhibition of human GR-ST cell growth in a cell viability assay. Homo sapiens 708.82 nM
SANGER: Inhibition of human LS-411N cell growth in a cell viability assay. Homo sapiens 836.81 nM
Inhibition of Mycobacterium avium DHFR Mycobacterium avium 150.0 nM
Inhibition of Pneumocystis jirovecii recombinant DHFR Pneumocystis jirovecii 130.0 nM
Inhibition of human recombinant DHFR Homo sapiens 400.0 nM
Antiplasmodial activity against wild type Plasmodium falciparum TM4 by [3H]-hypoxanthine incorporation assay Plasmodium falciparum 58.0 nM
Antimalarial activity against gametocytic stage of Plasmodium berghei infected in blood assessed as inhibition of ookinete formation at 10 uM after 24 hrs by Giemsa staining-based microscopic analysis relative to control Plasmodium berghei 50.0 %
Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysis relative to control Plasmodium falciparum 50.0 %
Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay Plasmodium falciparum 14.0 nM
Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum at 120 uM after 72 hrs by image-based HTS assay relative to control Plasmodium falciparum 100.0 %
Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum at 120 uM after 72 hrs by image-based HTS assay relative to control Plasmodium falciparum 40.0 %
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM Cricetulus griseus 72.59 %
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM Cricetulus griseus 107.42 %
Inhibition of mouse Mate1 transfected in HEK293 cells assessed as uptake of [14C]-TEA preincubated for 15 mins by liquid scintillation counting analysis Mus musculus 145.0 nM
Antibacterial activity against tachyzoite stage of Toxoplasma gondii PHdeltaHX infected in human TerT cells measured after 4 days Toxoplasma gondii 570.0 nM
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate Alamar blue assay Mycobacterium tuberculosis H37Rv 37.35 ug.mL-1
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 25 ug/ml after 7 days by microplate Alamar blue assay relative to control Mycobacterium tuberculosis H37Rv 26.7 %
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 50 ug/ml after 7 days by microplate Alamar blue assay relative to control Mycobacterium tuberculosis H37Rv 69.7 %
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 100 ug/ml after 7 days by microplate Alamar blue assay relative to control Mycobacterium tuberculosis H37Rv 95.6 %
Antimalarial activity against schizont stage of chloroquine-susceptible Plasmodium falciparum 3D7 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis Plasmodium falciparum 3D7 13.3 nM
Antimalarial activity against schizont stage of chloroquine-susceptible Plasmodium falciparum 3D7 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis Plasmodium falciparum 3D7 2.1 nM
Antimalarial activity against schizont stage of chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis Plasmodium falciparum 10.4 nM
Antimalarial activity against schizont stage of chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis Plasmodium falciparum 2.3 nM
Antimalarial activity against schizont stage of atovaquone-resistant Plasmodium falciparum Tm90C2b infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis Plasmodium falciparum 14.6 nM
Antimalarial activity against schizont stage of atovaquone-resistant Plasmodium falciparum Tm90C2b infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis Plasmodium falciparum 1.4 nM
Antitoxoplasma activity against Toxoplasma gondii RH tachyzoites isolated from human brain assessed as parasite growth inhibition after 24 hrs by hematoxylin-eosin staining based light microscopy Toxoplasma gondii RH 240.0 nM
Antitoxoplasma activity against Toxoplasma gondii RH tachyzoites isolated from human brain assessed as parasite growth inhibition after 48 hrs by hematoxylin-eosin staining based light microscopy Toxoplasma gondii RH 120.0 nM
Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth Enterococcus faecium 8.0 nM
Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth Lactobacillus casei 240.0 nM
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 after 72 hrs by SYBR I method Plasmodium falciparum NF54 28.26 nM
Antiplasmodial activity against Plasmodium falciparum SB1 after 72 hrs by SYBR I method Plasmodium falciparum 10.85 nM
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of parasite growth after 72 hrs by parasite LDH release assay Plasmodium falciparum D6 10.0 nM
Antiplasmodial activity against Plasmodium falciparum NF54 by SYBR-green based assay Plasmodium falciparum NF54 28.3 nM
Antiplasmodial activity against Plasmodium falciparum SB1-A6 harboring mutations conferring drug-resistance by SYBR-green based assay Plasmodium falciparum 10.9 nM
Antiplasmodial activity against Plasmodium falciparum NF54 by SYBR Green-based method Plasmodium falciparum NF54 28.0 nM
Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 by SYBR green-based assay Plasmodium falciparum NF54 28.0 nM
Antiparasitic activity against promastigote form of Leishmania mexicana MHOM/BZ/61/M379 at 100 uM after 24 hrs by haemocytometer Leishmania mexicana 50.0 %
ST_JUDE_LEISH: Cytotoxicity at 2uM final concentration against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro Leishmania mexicana 2.26 %
ST_JUDE_LEISH: Cytotoxicity at 2uM final concentration against transgenic Leishmania Mexicana promastigotes LmPfHT that are glucose transport deficient and complemented with the Plasmodium falciparum hexose transporter. Activity is measured by by DNA content using SYBR green in vitro Leishmania mexicana 3.31 %
ST_JUDE_LEISH: Cytotoxicity at 2uM final concentration against transgenic Leishmania Mexicana promastigotes LmGT2 that are glucose transport deficient and complemented with the L. Mexicana glucose transporter 2. Activity is measured by by DNA content using SYBR green in vitro Leishmania mexicana 3.36 %
PubChem BioAssay. nuclear beta catenin stimulation in WNT3A conditioned C2C12 cells-IC50. (Class of assay: confirmatory) None 860.0 nM
PubChem BioAssay. alkaline phosphatase stimulation in WNT3A conditioned C2C12 cells-IC50. (Class of assay: confirmatory) None 67.7 nM
Antimalarial activity against Plasmodium falciparum 3D7A infected in red blood cells assessed as inhibition of parasite growth after 24 hrs by [3H]hypoxanthine incorporation assay Plasmodium falciparum 68.0 nM
Antiparasitic activity against Toxoplasma gondii RH tachyzoite expressing beta-galactosidase assessed as inhibition of tachyzoite invasion into human foreskin fibroblast host cells after 96 hrs by colorimetric microtitre assay Toxoplasma gondii RH 340.0 nM
Cytotoxicity against HEK293 cells assessed as cell viability after 72 hrs by resazurin-based plate reader analysis Homo sapiens 4.22 nM
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis Plasmodium falciparum 3D7 2.5 nM
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth at 40 uM after 72 hrs by DAPI staining-based confocal microscopic analysis Plasmodium falciparum Dd2 62.0 %
Antimalarial activity against Plasmodium falciparum 3D7 incubated for 72 hours by DAPI-staining based confocal imaging analysis Plasmodium falciparum 3D7 8.45 nM
Antimalarial activity against Plasmodium falciparum Dd2 incubated for 72 hours by DAPI-staining based confocal imaging analysis Plasmodium falciparum Dd2 120.0 nM
Cytotoxicity against HEK293 cells by alamar blue assay Homo sapiens 8.07 nM
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 Toxoplasma gondii 230.0 nM
Antiplasmodial activity against pyrimethamine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes incubated for 50 hrs by SYBR green 1 dye based fluorescence assay Plasmodium falciparum 3D7 47.0 nM
Inhibition of trophozoite stage of Plasmodium falciparum DHFR assessed as reduction in NADPH depletion at 50 uM incubated for 30 mins followed by NADPH addition measured for 30 mins at 15 secs interval by UV/Vis spectrophotometric analysis Plasmodium falciparum 25.0 %
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method Plasmodium falciparum 3D7 2.5 nM
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay Plasmodium falciparum D6 9.0 nM
Antimalarial activity against Plasmodium falciparum Plasmodium falciparum 0.25 ug.mL-1
Inhibition of bovine liver DHFR using FH2 as substrate preincubated for 2 mins followed by substrate addition in presence of NADPH Bos taurus 0.035 ug.mL-1
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay Plasmodium falciparum D6 10.0 nM
Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 measured after 72 hrs by DAPI staining based high throughput screening assay Plasmodium falciparum 3D7 8.0 nM
Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay Chlorocebus sabaeus 6.25 ug.mL-1
Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method Plasmodium falciparum NF54 45.0 nM
Antimalarial activity against Plasmodium falciparum T9/94 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method Plasmodium falciparum 38.0 nM
Inhibition of bovine liver DHFR Bos taurus 100.7 nM
Inhibition of human DHFR using dihydrofolate as substrate after 180 secs by spectrophotometric analysis Homo sapiens 470.0 nM
Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Respiratory syncytial virus 750.0 nM
Inhibition of bovine liver DHFR pre-incubated 2 mins before dihydrofolic acid substrate addition and measured over 10 mins in presence of NADPH Bos taurus 100.7 nM
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method Plasmodium falciparum 3D7 6.0 nM
Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay Homo sapiens 690.0 nM
Antiplasmodial activity against drug-sensitive blood stage Plasmodium falciparum 3D7 by SYBR green 1 staining based fluorescence assay Plasmodium falciparum 3D7 30.0 nM
Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method Plasmodium falciparum 3D7 8.0 nM
Inhibition of Plasmodium falciparum DHFR Plasmodium falciparum 58.0 nM
Inhibition of Plasmodium falciparum DHFR using DHF as substrate preincubated for 15 mins followed DHF addition measured after 15 mins by spectrophotometric method Plasmodium falciparum 25.5 nM
Antimalarial activity against Plasmodium falciparum in infected in human RBC Plasmodium falciparum 0.25 ug.mL-1
Inhibition of bovine liver DHFR using FH2 as substrate preincubated for 2 mins followed by substrate addition Bos taurus 0.035 ug.mL-1
Antiplasmodial activity against Plasmodium falciparum 3D7 after 3 days by SYBR green1 dye based assay Plasmodium falciparum 3D7 33.0 nM
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging Homo sapiens 57.63 %
Inhibition of Plasmodium falciparum TM4/8.2 wild type DHFR NCSI haplotype Plasmodium falciparum 0.6 nM
Inhibition of Plasmodium falciparum K1CB1 DHFR NRNI haplotype C59R/S108N double mutant Plasmodium falciparum 53.9 nM
Inhibition of Plasmodium falciparum W2 DHFR IRNI haplotype N51I/C59R/S108N triple mutant Plasmodium falciparum 67.1 nM
Inhibition of Plasmodium falciparum CSL-2 DHFR NRNL haplotype C59R/S108N/I164L triple mutant Plasmodium falciparum 112.0 nM
Inhibition of Plasmodium falciparum V1/S DHFR IRNL haplotype N51I/C59R/S108N/I164L quadruple mutant Plasmodium falciparum 390.0 nM
Inhibition of human DHFR Homo sapiens 28.2 nM
Antiplasmodial activity against Plasmodium falciparum TM4/8.2 harboring wild type DHFR NCSI haplotype Plasmodium falciparum 80.0 nM
Anti-plasmodial activity against chloroquine resistant Plasmodium falciparum RKL9 infected in human erythrocytes after 24 hrs by Giemsa staining-based method Plasmodium falciparum 12.46 nM
Inhibition of bovine liver DHFR using FH2 as substrate incubated for 2 mins followed by substrate addition Bos taurus 0.035 ug.mL-1
Antimalarial activity against Plasmodium falciparum FCR3 infected in human erythrocytes by Giemsa staining analysis Plasmodium falciparum 0.25 ug.mL-1 Antimalarial activity against Plasmodium falciparum FCR3 infected in human erythrocytes by Giemsa staining analysis Plasmodium falciparum 250.03 nM
Antiparasitic activity against Toxoplasma gondii RH transfected with fluorescent transgene dTom Toxoplasma gondii 800.0 nM
Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis Plasmodium falciparum 5.1 nM
Anti-plasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 72 hrs by SYBR green dye based fluorescence assay Plasmodium falciparum 35.0 nM
Inhibition of N-terminal His-tagged Trypanosoma brucei pteridine reductase 1 using di-hydrobiopterine as substrate measured at 1 min interval for 50 mins in presence of NADPH Trypanosoma brucei 90.0 nM
Competitive inhibition of wild type Plasmodium falciparum dihydrofolate reductase expressed in Escherichia coli BL21(DE3)pLysS using dihydrofolate as substrate in presence of NADPH by UV-vis spectrophotometry analysis Plasmodium falciparum 0.6 nM
Competitive inhibition of Plasmodium falciparum dihydrofolate reductase N51I/C59R/S108N/I164L quadruple mutant expressed in Escherichia coli BL21(DE3)pLysS using dihydrofolate as substrate in presence of NADPH by UV-vis spectrophotometry analysis Plasmodium falciparum 385.0 nM
Inhibition of human dihydrofolate reductase using dihydrofolate as substrate in presence of NADPH by UV-vis spectrophotometry analysis Homo sapiens 28.3 nM
Antimalarial activity against Plasmodium falciparum TM4/8.2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting method Plasmodium falciparum 80.0 nM
Antiplasmodial activity against Plasmodium falciparum 3D7A erythrocytic stage assessed as reduction in [3H]hypoxanthine incorporation preincubated for 24 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by microbeta scintillation counting method Plasmodium falciparum 100.0 nM
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 Toxoplasma gondii 139.0 nM
Parasiticidal activity against bacterial beta-galactosidase expressing Toxoplasma gondii I RH 2F clone infected in HFF cells after 72 hrs Toxoplasma gondii RH 680.0 nM
Inhibition of human DHFR Homo sapiens 760.0 nM
Antiplasmodial activity against chloroquine/antifolate-sensitive Plasmodium falciparum TM4 infected in human RBC incubated for 18 to 20 hrs by microdilution radioisotope method Plasmodium falciparum 80.0 nM
Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis Plasmodium falciparum 7.7 nM
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate Severe acute respiratory syndrome coronavirus 2 15.51 % SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate Severe acute respiratory syndrome coronavirus 2 15.45 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 9.02 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.1 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 9.02 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.1 %
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite rowth incubated for 72 hrs by DAPI staining based fluorescence assay Plasmodium falciparum 2.5 nM
Inhibition of Mycobacterium smegmatis ATCC 607 dihydrofolic reductase Mycobacterium smegmatis 75.0 nM
Antimalarial activity against erythrocytic stage of Plasmodium falciparum 3D7 incubated for 50 hrs Plasmodium falciparum 11.0 nM
Antimalarial activity against Plasmodium falciparum 3D7 asexual forms incubated for 72 hrs by luminescence method Plasmodium falciparum 4.35 nM
Antimalarial activity against chloroquine-sensitive synchronized ring stage of Plasmodium falciparum 3D7 incubated for 48 to 52 hrs by SYBR green 1 dye based assay Plasmodium falciparum 18.0 nM
Antimalarial activity against chloroquine-sensitive plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition measured after 72 hrs by SYBR green dye based fluorescence analysis Plasmodium falciparum 4.0 nM
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 72 hrs by DAPI-staining based imaging analysis Plasmodium falciparum 6.0 nM
Antimalarial activity against Plasmodium falciparum 3D7 assessed as reduction in parasite growth measured after 72 hrs by Monash assay based fluorescence analysis Plasmodium falciparum 44.0 nM
Antimalarial activity against synchronous ring stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis Plasmodium falciparum 4.7 nM

Cross References

Resources Reference
ChEBI 8673
ChEMBL CHEMBL36
DrugBank DB00205
DrugCentral 2332
FDA SRS Z3614QOX8W
Human Metabolome Database HMDB0014350
Guide to Pharmacology 4800
KEGG C07391
PDB CP6
PharmGKB PA451193
PubChem 4993
SureChEMBL SCHEMBL25129
ZINC ZINC000000057464
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