Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | dihydrofolate reductase | Starlite/ChEMBL | References |
Candida albicans | dihydrofolate reductase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | dihydrofolate reductase | 187 aa | 202 aa | 29.7 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Mycobacterium leprae | DIHYDROFOLATE REDUCTASE DFRA (DHFR) (TETRAHYDROFOLATE DEHYDROGENASE) | 0.0415 | 0.5 | 0.5 |
Echinococcus multilocularis | dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Schistosoma mansoni | dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Chlamydia trachomatis | dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Brugia malayi | Dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Mycobacterium tuberculosis | Dihydrofolate reductase DfrA (DHFR) (tetrahydrofolate dehydrogenase) | 0.0415 | 0.5 | 0.5 |
Loa Loa (eye worm) | dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Mycobacterium ulcerans | dihydrofolate reductase DfrA | 0.0415 | 0.5 | 0.5 |
Echinococcus granulosus | dihydrofolate reductase | 0.0415 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 4.4 nM | Activity was evaluated against HCT-8 tumor cells | ChEMBL. | 8632413 |
IC50 (functional) | = 4.4 nM | Activity was evaluated against HCT-8 tumor cells | ChEMBL. | 8632413 |
Inhibition (functional) | = 0 % | GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 LDH activity, using an LDH reporter assay. Test compounds present at 2uM | ChEMBL. | 20485427 |
Inhibition (functional) | = 42.64 % | 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 | ChEMBL. | No reference |
Inhibition (functional) | = 46.31 % | 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 | ChEMBL. | No reference |
Inhibition (functional) | = 54.9 % | 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 | ChEMBL. | No reference |
Inhibition (functional) | = 70 % | GSK_TCMDC: Percent inhibition of human HepG2 cell line. Test compounds present at 10uM. | ChEMBL. | 20485427 |
Inhibition (functional) | = 73 % | 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 | ChEMBL. | 20485427 |
Inhibition (functional) | = 100 % | 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 | ChEMBL. | 20485427 |
Inhibition frequency index (IFI) (functional) | = 8.84 | Inhibition Frequency Index (IFI) | GSK. | 20485427 |
Ki (binding) | < 0.11 nM | Inhibition of Dihydrofolate reductase enzyme from Candida albicans | ChEMBL. | 8632413 |
Ki (binding) | < 0.11 nM | Inhibition of Dihydrofolate reductase enzyme from Candida albicans | ChEMBL. | 8632413 |
Ki (binding) | = 0.4 nM | Inhibition of human recombinant Dihydrofolate reductase enzyme | ChEMBL. | 8632413 |
Ki (binding) | = 0.4 nM | Inhibition of human recombinant Dihydrofolate reductase enzyme | ChEMBL. | 8632413 |
MIC (functional) | > 0.1 ug ml-1 | Minimum inhibitory concentration evaluated against Candida albicans | ChEMBL. | 8632413 |
MIC (functional) | > 0.1 ug ml-1 | Minimum inhibitory concentration evaluated against Candida albicans | ChEMBL. | 8632413 |
Percent growth inhibition (functional) | = -1 % | Percent inhibition of P. falciparum lactate dehydrogenase activity (at 2 uM) | GSK. | 20485427 |
Percent growth inhibition (functional) | = 70 % | Percent inhibition of HepG2 growth (at 10 uM) | GSK. | 20485427 |
Percent growth inhibition (functional) | = 73 % | Percent inhibition of P. falciparum Dd2 growth (at 2 uM) | GSK. | 20485427 |
Percent growth inhibition (functional) | = 102 % | Percent inhibition of P. falciparum 3D7 growth (at 2 uM) | GSK. | 20485427 |
XC50 (functional) | = 8.49 | XC50 determination of P. falciparum 3D7 growth | GSK. | 20485427 |
XC50 (functional) | = 0.0032 uM | GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 in whole erythrocytes, using parasite LDH activity as an index of growth. | ChEMBL. | 20485427 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 8632413 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
2 literature references were collected for this gene.