An EC 1.5.1.* (oxidoreductase acting on donor CH-NH group, NAD(+) or NADP(+) as acceptor) inhibitor that interferes with the action of dihydrofolate reductase (EC 1.5.1.3).
| Member | Definition | Class |
|---|
| 10-propargyl-10-deazaaminopterin | A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma. | pralatrexate |
| aminopterin | | 4-aminofolic acid |
| brodimoprim | An aminopyrimidine that is 2,4-diaminopyrimidine in which the hydrogen at position 5 has been replaced by a 4-bromo-3,5-dimethoxybenzyl group. | brodimoprim |
| cycloguanil | A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil. | cycloguanil |
| methotrexate | | methotrexate |
| o-(chloroacetylcarbamoyl)fumagillol | A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative. | O-(chloroacetylcarbamoyl)fumagillol |
| pemetrexed | An N-acylglutamic acid in which the N-acyl group is specified as 4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | pemetrexed |
| proguanil | A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells. | proguanil |
| pyrimethamine | An aminopyrimidine that is pyrimidine-2,4-diamine which is substituted at position 5 by a p-chlorophenyl group and at position 6 by an ethyl group. It is a folic acid antagonist used as an antimalarial or with a sulfonamide to treat toxoplasmosis. | pyrimethamine |
| triclosan | An aromatic ether that is phenol which is substituted at C-5 by a chloro group and at C-2 by a 2,4-dichlorophenoxy group. It is widely used as a preservative and antimicrobial agent in personal care products such as soaps, skin creams, toothpaste and deodorants as well as in household items such as plastic chopping boards, sports equipment and shoes. | triclosan |
| trimethoprim | An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | trimethoprim |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 22.8478 | 1 | 3 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 14.6198 | 2 | 12 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 40.2352 | 2 | 4 |
| acid sphingomyelinase | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 51.8874 | 2 | 4 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 33.1347 | 1 | 5 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 19.6222 | 1 | 2 |
| Alpha-synuclein | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 27.3585 | 10 | 42 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 47.8507 | 2 | 2 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 14.6701 | 2 | 2 |
| Ataxin-2 | Homo sapiens (human) | Potency | 18.5137 | 1 | 6 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 37.9330 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 19.8947 | 2 | 7 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 9.9779 | 2 | 4 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 55.7595 | 1 | 1 |
| caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 62.5632 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 55.7595 | 1 | 1 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 62.5632 | 1 | 1 |
| Caspase-7 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 18.9270 | 3 | 20 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 5.1832 | 2 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 29.9033 | 1 | 2 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 34.6344 | 2 | 4 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 15.8146 | 2 | 2 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 24.0682 | 2 | 2 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 77.2179 | 1 | 3 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 15.8146 | 2 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 28.1200 | 1 | 2 |
| ClpP | Bacillus subtilis | Potency | 23.7358 | 1 | 2 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.4730 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.6807 | 1 | 3 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 8.9716 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 9.6845 | 2 | 7 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 17.0933 | 1 | 3 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 36.4737 | 1 | 2 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 64.9062 | 1 | 3 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 46.7791 | 1 | 2 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 2.3170 | 1 | 2 |
| endonuclease IV | Escherichia coli | Potency | 0.8913 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 27.8578 | 10 | 47 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 41.4983 | 3 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 9.6590 | 10 | 56 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 7.6667 | 1 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 1.4517 | 4 | 16 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 24.3430 | 4 | 12 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 27.0147 | 1 | 4 |
| G | Vesicular stomatitis virus | Potency | 3.4730 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 10.0476 | 1 | 4 |
| geminin | Homo sapiens (human) | Potency | 7.1232 | 2 | 9 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 25.2970 | 3 | 15 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 26.5434 | 3 | 8 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 27.0570 | 1 | 6 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 21.7311 | 2 | 8 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 25.9042 | 1 | 4 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 32.2842 | 2 | 11 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.4730 | 1 | 2 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 42.3490 | 2 | 5 |
| IDH1 | Homo sapiens (human) | Potency | 6.7742 | 1 | 4 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.4730 | 1 | 4 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 6.3446 | 1 | 2 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 6.3446 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 22.4467 | 2 | 4 |
| interleukin 8 | Homo sapiens (human) | Potency | 74.9780 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 5.6434 | 2 | 6 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 1 | 1 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 17.5491 | 2 | 5 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 1 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.2512 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 11.3328 | 3 | 21 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 6.5201 | 1 | 2 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 45.3206 | 2 | 5 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 10.1138 | 3 | 16 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Parkin | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 23.9341 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 5.4473 | 2 | 4 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 19.8830 | 5 | 17 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 41.9395 | 4 | 9 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 50.1187 | 1 | 1 |
| PINK1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 0.7079 | 1 | 1 |
| polyprotein | Zika virus | Potency | 27.0146 | 1 | 4 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 35.6300 | 2 | 9 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 50.1187 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 16.6112 | 2 | 10 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 23.3427 | 2 | 10 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 29.1114 | 3 | 7 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 17.9921 | 3 | 13 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 41.1092 | 3 | 4 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 41.1092 | 3 | 4 |
| Smad3 | Homo sapiens (human) | Potency | 26.6320 | 1 | 2 |
| snurportin-1 | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 13.8826 | 1 | 4 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 13.1348 | 1 | 5 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 18.3701 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 6.1169 | 2 | 28 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 34.8515 | 3 | 5 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 10.1110 | 3 | 23 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 22.0001 | 5 | 5 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 33.1886 | 2 | 2 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 38.7088 | 1 | 1 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 0.7079 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 0.7079 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 48.0224 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 29.4781 | 2 | 10 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 30.2308 | 3 | 8 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 27.0570 | 1 | 6 |
| Vpr | Human immunodeficiency virus 1 | Potency | 56.2341 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 3-oxoacyl-[acyl-carrier-protein] synthase 3 | Escherichia coli | IC50 | 850.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 | 7.5006 | 1 | 2 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | IC50 | 86.8167 | 3 | 3 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | IC50 | 0.0146 | 2 | 2 |
| 5-hydroxytryptamine receptor 7 | Cavia porcellus (domestic guinea pig) | IC50 | 56.8000 | 1 | 2 |
| 6-phosphogluconate dehydrogenase, decarboxylating | Homo sapiens (human) | Ki | 136.7000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| ATP-binding cassette sub-family C member 3 | Rattus norvegicus (Norway rat) | Ki | 90.0000 | 1 | 1 |
| Beta-hexosaminidase subunit alpha | Homo sapiens (human) | IC50 | 11.0833 | 6 | 6 |
| Beta-hexosaminidase subunit beta | Homo sapiens (human) | IC50 | 10.2286 | 7 | 7 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Cryptosporidium parvum | IC50 | 507.0000 | 1 | 2 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Leishmania major | IC50 | 20.5000 | 1 | 1 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium berghei ANKA | IC50 | 0.1200 | 5 | 5 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum 3D7 | IC50 | 2.4800 | 1 | 1 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum K1 | IC50 | 31.3399 | 10 | 17 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Toxoplasma gondii | IC50 | 40.1226 | 67 | 125 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Trypanosoma cruzi | IC50 | 0.1100 | 1 | 1 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Leishmania major | Ki | 0.0601 | 2 | 2 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum 3D7 | Ki | 0.0008 | 1 | 1 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum K1 | Ki | 0.5010 | 27 | 47 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Plasmodium vivax (malaria parasite P. vivax) | Ki | 0.0016 | 1 | 2 |
| Bifunctional purine biosynthesis protein ATIC | Homo sapiens (human) | IC50 | 6.6933 | 2 | 3 |
| Bifunctional purine biosynthesis protein ATIC | Homo sapiens (human) | Ki | 100.4400 | 1 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 446.1500 | 4 | 8 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 118.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Canalicular multispecific organic anion transporter 1 | Rattus norvegicus (Norway rat) | Ki | 341.3333 | 3 | 3 |
| Carbonyl reductase [NADPH] 1 | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| Carbonyl reductase [NADPH] 1 | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| cGMP-dependent 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 39.6500 | 1 | 2 |
| Chain A, Dihydrofolate reductase | Bacillus anthracis | IC50 | 77,200.0000 | 1 | 1 |
| Chain A, Dihydrofolate reductase | Homo sapiens (human) | Ki | 0.6050 | 1 | 4 |
| Chain A, dihydrofolate reductase (DHFR) | Bacillus anthracis | IC50 | 77,200.0000 | 1 | 1 |
| Chain A, enoyl-acyl carrier reductase | Plasmodium falciparum (malaria parasite P. falciparum) | Ki | 0.0500 | 1 | 3 |
| Chain A, Thymidylate Synthase | Escherichia coli | Ki | 0.1090 | 1 | 2 |
| Chain A, Thymidylate Synthase | Homo sapiens (human) | Ki | 0.1090 | 1 | 1 |
| Chain C, enoyl-acyl carrier reductase | Plasmodium falciparum (malaria parasite P. falciparum) | Ki | 0.0500 | 1 | 3 |
| Cytochrome P450 11B1, mitochondrial | Bos taurus (cattle) | IC50 | 0.0012 | 2 | 5 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 51.5000 | 1 | 1 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 1 |
| Dihydrofolate reductase | Candida albicans | IC50 | 21.2620 | 5 | 6 |
| Dihydrofolate reductase | Enterococcus faecium | IC50 | 0.0014 | 1 | 1 |
| Dihydrofolate reductase | Escherichia coli K-12 | IC50 | 174.1020 | 47 | 96 |
| Dihydrofolate reductase | Gallus gallus (chicken) | IC50 | 296.0218 | 5 | 5 |
| Dihydrofolate reductase | Homo sapiens (human) | IC50 | 70.0169 | 110 | 186 |
| Dihydrofolate reductase | Lacticaseibacillus casei | IC50 | 17.7979 | 32 | 39 |
| Dihydrofolate reductase | Lactococcus lactis subsp. lactis Il1403 | IC50 | 0.4500 | 1 | 1 |
| Dihydrofolate reductase | Mus musculus (house mouse) | IC50 | 0.0304 | 12 | 17 |
| Dihydrofolate reductase | Mycobacterium tuberculosis H37Rv | IC50 | 22.0130 | 4 | 4 |
| Dihydrofolate reductase | Neisseria gonorrhoeae | IC50 | 0.4500 | 2 | 2 |
| Dihydrofolate reductase | Pneumocystis carinii | IC50 | 186.4746 | 46 | 76 |
| Dihydrofolate reductase | Rattus norvegicus (Norway rat) | IC50 | 2,307.1609 | 58 | 82 |
| Dihydrofolate reductase | Saccharomyces cerevisiae S288C | IC50 | 12.0000 | 1 | 1 |
| Dihydrofolate reductase | Staphylococcus aureus | IC50 | 982.6437 | 10 | 17 |
| Dihydrofolate reductase | Streptococcus pneumoniae TIGR4 | IC50 | 64.1815 | 2 | 6 |
| Dihydrofolate reductase | Escherichia coli K-12 | Ki | 8.7041 | 17 | 20 |
| Dihydrofolate reductase | Gallus gallus (chicken) | Ki | 59.5946 | 3 | 4 |
| Dihydrofolate reductase | Homo sapiens (human) | Ki | 4.4879 | 30 | 42 |
| Dihydrofolate reductase | Lacticaseibacillus casei | Ki | 3.5147 | 4 | 5 |
| Dihydrofolate reductase | Mus musculus (house mouse) | Ki | 0.2157 | 19 | 23 |
| Dihydrofolate reductase | Pneumocystis carinii | Ki | 48.6808 | 3 | 8 |
| Dihydrofolate reductase | Staphylococcus aureus | Ki | 0.1833 | 14 | 15 |
| Dihydrofolate reductase | Bacillus anthracis | IC50 | 32.7096 | 5 | 7 |
| Dihydrofolate reductase | Bos taurus (cattle) | IC50 | 1,018.0999 | 14 | 14 |
| Dihydrofolate reductase | Mycobacterium avium | IC50 | 33.5633 | 9 | 9 |
| Dihydrofolate reductase | Pneumocystis jirovecii | IC50 | 0.0920 | 1 | 1 |
| Dihydrofolate reductase | Bacillus anthracis | Ki | 12.7600 | 3 | 3 |
| Dihydrofolate reductase | Salmonella enterica subsp. enterica serovar Typhi | Ki | 0.0075 | 1 | 2 |
| Dihydrofolate reductase type 1 | Escherichia coli | IC50 | 0.2500 | 2 | 2 |
| Dihydrofolate reductase type 1 from Tn4003 | Staphylococcus aureus | IC50 | 109.5308 | 1 | 4 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 | 2.1225 | 3 | 4 |
| Dipeptidyl peptidase 4 | Rattus norvegicus (Norway rat) | IC50 | 2.7000 | 1 | 1 |
| DNA gyrase subunit A | Escherichia coli K-12 | IC50 | 1,000.0000 | 1 | 1 |
| DNA gyrase subunit B | Escherichia coli K-12 | IC50 | 1,000.0000 | 1 | 1 |
| dual specificity protein phosphatase 3 | Homo sapiens (human) | IC50 | 80.0000 | 2 | 2 |
| Endoplasmic reticulum chaperone BiP | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | IC50 | 2.8712 | 8 | 8 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | Ki | 0.2100 | 4 | 4 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Francisella tularensis subsp. tularensis SCHU S4 | IC50 | 4.3300 | 5 | 5 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] FabI | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 0.5000 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] FabI | Escherichia coli K-12 | IC50 | 2.9579 | 8 | 12 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] FabI | Haemophilus influenzae Rd KW20 | IC50 | 7.6425 | 2 | 4 |
| Enoyl-[acyl-carrier-protein] reductase [NADPH] FabI | Staphylococcus aureus subsp. aureus MRSA252 | IC50 | 2.6049 | 10 | 14 |
| Enoyl-[acyl-carrier-protein] reductase [NADPH] FabI | Staphylococcus aureus subsp. aureus MRSA252 | Ki | 0.0000 | 1 | 1 |
| Enoyl-ACP reductase II | Streptococcus pneumoniae | IC50 | 32.0000 | 2 | 2 |
| Enoyl-acyl carrier reductase | Toxoplasma gondii | IC50 | 0.0167 | 3 | 3 |
| Enoyl-acyl-carrier protein reductase | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.0872 | 8 | 8 |
| Enoyl-acyl-carrier protein reductase | Plasmodium falciparum (malaria parasite P. falciparum) | Ki | 0.0554 | 17 | 17 |
| Fatty-acid amide hydrolase 1 | Mus musculus (house mouse) | IC50 | 0.0800 | 1 | 1 |
| Folate receptor alpha | Homo sapiens (human) | IC50 | 0.2936 | 6 | 12 |
| Folate receptor beta | Homo sapiens (human) | IC50 | 0.2185 | 6 | 10 |
| Folylpolyglutamate synthase, mitochondrial | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| Folylpolyglutamate synthase, mitochondrial | Mus musculus (house mouse) | Ki | 91.8000 | 1 | 2 |
| Glucose-6-phosphate 1-dehydrogenase | Homo sapiens (human) | Ki | 91.0000 | 1 | 1 |
| Histidine decarboxylase | Rattus norvegicus (Norway rat) | IC50 | 0.0014 | 1 | 1 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 1 |
| Low molecular weight phosphotyrosine protein phosphatase | Homo sapiens (human) | IC50 | 15.6150 | 2 | 2 |
| low molecular weight phosphotyrosine protein phosphatase isoform c | Homo sapiens (human) | IC50 | 28.2500 | 2 | 2 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | IC50 | 2.7300 | 1 | 1 |
| Methionine aminopeptidase 2 | Homo sapiens (human) | IC50 | 0.5930 | 4 | 4 |
| Methionine aminopeptidase 2 | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 2.8000 | 1 | 1 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Mus musculus (house mouse) | Ki | 0.1450 | 1 | 1 |
| Multidrug resistance associated protein | Homo sapiens (human) | Ki | 1,200.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| NH(3)-dependent NAD(+) synthetase | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 1.0000 | 1 | 1 |
| nuclear receptor coactivator 1 isoform 1 [Homo sapiens] | Homo sapiens (human) | IC50 | 35.8790 | 2 | 2 |
| nuclear receptor coactivator 3 isoform a | Homo sapiens (human) | IC50 | 18.0450 | 2 | 2 |
| Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | IC50 | 0.5850 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 239.8830 | 3 | 3 |
| Protein-arginine deiminase type-4 | Homo sapiens (human) | IC50 | 8,750.0000 | 1 | 2 |
| Proton-coupled folate transporter | Homo sapiens (human) | IC50 | 0.0516 | 5 | 8 |
| Proton-coupled folate transporter | Homo sapiens (human) | Ki | 0.6776 | 7 | 7 |
| Pteridine reductase 1 | Leishmania major | IC50 | 13.6000 | 1 | 1 |
| Pteridine reductase 1 | Leishmania major | Ki | 0.1095 | 2 | 2 |
| Reduced folate transporter | Homo sapiens (human) | IC50 | 0.0611 | 5 | 8 |
| Reduced folate transporter | Homo sapiens (human) | Ki | 3.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 75.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 75.0000 | 1 | 1 |
| Serine hydroxymethyltransferase, cytosolic | Homo sapiens (human) | Ki | 79.2333 | 3 | 3 |
| Solute carrier family 22 member 1 | Mus musculus (house mouse) | Ki | 3.6000 | 1 | 1 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 40.3500 | 2 | 3 |
| Solute carrier family 22 member 20 | Mus musculus (house mouse) | Ki | 599.7800 | 1 | 2 |
| Solute carrier family 22 member 6 | Mus musculus (house mouse) | Ki | 896.1255 | 1 | 2 |
| Solute carrier organic anion transporter family member 1A3 | Rattus norvegicus (Norway rat) | Ki | 0.5000 | 1 | 1 |
| Substance-K receptor | Rattus norvegicus (Norway rat) | Ki | 0.0717 | 1 | 1 |
| Thymidylate synthase | Escherichia coli K-12 | IC50 | 46.1546 | 3 | 18 |
| Thymidylate synthase | Homo sapiens (human) | IC50 | 35.6582 | 28 | 49 |
| Thymidylate synthase | Lacticaseibacillus casei | IC50 | 121.2143 | 14 | 14 |
| Thymidylate synthase | Mus musculus (house mouse) | IC50 | 20.0000 | 2 | 2 |
| Thymidylate synthase | Homo sapiens (human) | Ki | 0.2357 | 4 | 4 |
| Thymidylate synthase | Lacticaseibacillus casei | Ki | 0.5500 | 1 | 1 |
| Thymidylate synthase | Mus musculus (house mouse) | Ki | 22.6700 | 2 | 2 |
| Thymidylate synthase | Escherichia coli | IC50 | 110.6812 | 13 | 16 |
| Thymidylate synthase | Escherichia coli LF82 | IC50 | 47.0000 | 1 | 2 |
| Thymidylate synthase | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| Toll-like receptor 4 | Homo sapiens (human) | IC50 | 1.0400 | 1 | 1 |
| transactivating tegument protein VP16 [Human herpesvirus 1] | Human alphaherpesvirus 1 (Herpes simplex virus type 1) | IC50 | 35.8790 | 2 | 2 |
| Transthyretin | Homo sapiens (human) | IC50 | 53.5000 | 1 | 1 |
| Trifunctional purine biosynthetic protein adenosine-3 | Homo sapiens (human) | IC50 | 6.2726 | 7 | 8 |
| Trifunctional purine biosynthetic protein adenosine-3 | Mus musculus (house mouse) | IC50 | 20.0000 | 5 | 5 |
| Trifunctional purine biosynthetic protein adenosine-3 | Homo sapiens (human) | Ki | 0.6113 | 4 | 4 |
| tyrosine-protein phosphatase non-receptor type 22 isoform 1 | Homo sapiens (human) | IC50 | 80.0000 | 2 | 2 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 34.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | ID50 | 0.0450 | 1 | 2 |
| ATP-binding cassette sub-family C member 11 | Homo sapiens (human) | Km | 957.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Rattus norvegicus (Norway rat) | Km | 8.1000 | 2 | 2 |
| Beta-hexosaminidase subunit alpha | Homo sapiens (human) | Activity | 30.0000 | 1 | 1 |
| Bifunctional dihydrofolate reductase-thymidylate synthase | Toxoplasma gondii | Activity | 2.8000 | 1 | 1 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | Km | 2,560.0000 | 3 | 3 |
| Canalicular multispecific organic anion transporter 1 | Rattus norvegicus (Norway rat) | Km | 296.0000 | 1 | 1 |
| Dihydrofolate reductase | Pneumocystis carinii | Activity | 13.0000 | 1 | 1 |
| Dihydrofolate reductase | Rattus norvegicus (Norway rat) | Activity | 180.0000 | 1 | 1 |
| Dihydrofolate reductase | Homo sapiens (human) | IC80 | 1.4400 | 1 | 1 |
| Dihydrofolate reductase | Lacticaseibacillus casei | ID50 | 0.0154 | 6 | 6 |
| Dihydrofolate reductase | Mus musculus (house mouse) | ID50 | 0.0181 | 7 | 8 |
| Dihydrofolate reductase | Escherichia coli K-12 | Ratio | 0.0009 | 4 | 4 |
| Dihydrofolate reductase | Mycobacterium avium | Activity | 0.3000 | 1 | 1 |
| Dihydrofolate reductase type 1 | Escherichia coli | C50 | 550,000.0000 | 1 | 1 |
| Folylpolyglutamate synthase, mitochondrial | Mus musculus (house mouse) | Concentration | 47.0000 | 1 | 2 |
| Folylpolyglutamate synthase, mitochondrial | Homo sapiens (human) | Km | 18.6321 | 12 | 14 |
| Folylpolyglutamate synthase, mitochondrial | Mus musculus (house mouse) | Km | 5,866,728.3333 | 2 | 3 |
| Folylpolyglutamate synthase, mitochondrial | Homo sapiens (human) | Vmax | 0.9100 | 1 | 2 |
| heat shock protein 90, putative | Plasmodium falciparum 3D7 | AC50 | 7.5440 | 1 | 1 |
| heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | AC50 | 7.8470 | 1 | 1 |
| Multidrug resistance associated protein | Homo sapiens (human) | Km | 768.6667 | 3 | 3 |
| Multidrug resistance-associated protein 1 | Homo sapiens (human) | Km | 1,540.0000 | 2 | 2 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | Km | 1,300.0000 | 1 | 1 |
| Proton-coupled folate transporter | Homo sapiens (human) | K | 0.1570 | 2 | 2 |
| Solute carrier family 22 member 11 | Homo sapiens (human) | Km | 17.8000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | Km | 553.8000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Km | 16.0000 | 2 | 2 |
| Solute carrier organic anion transporter family member 1A3 | Rattus norvegicus (Norway rat) | Km | 1.6333 | 3 | 3 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Km | 24.7000 | 1 | 1 |
| twin arginine protein translocation system - TatA protein | Escherichia coli str. K-12 substr. MG1655 | AC50 | 1.0600 | 1 | 1 |