An EC 2.1.2.* (hydroxymethyl-, formyl- and related transferases) inhibitor that interferes with the action of phosphoribosylglycinamide formyltransferase (EC 2.1.2.2).
ChEBI ID: 63721
| Member | Definition | Class |
|---|---|---|
| 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 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 46 (1.91) | 18.2507 |
| 2000's | 521 (21.63) | 29.6817 |
| 2010's | 1,419 (58.90) | 24.3611 |
| 2020's | 423 (17.56) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 657 (26.61%) | 5.53% |
| Reviews | 362 (14.66%) | 6.00% |
| Case Studies | 288 (11.66%) | 4.05% |
| Observational | 28 (1.13%) | 0.25% |
| Other | 1,134 (45.93%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.3903 | 4 | 4 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 38.7088 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bifunctional dihydrofolate reductase-thymidylate synthase | Toxoplasma gondii | IC50 | 2.4780 | 15 | 15 |
| Bifunctional purine biosynthesis protein ATIC | Homo sapiens (human) | IC50 | 0.0700 | 1 | 1 |
| Bifunctional purine biosynthesis protein ATIC | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
| Chain A, Thymidylate Synthase | Escherichia coli | Ki | 0.1090 | 1 | 2 |
| Chain A, Thymidylate Synthase | Homo sapiens (human) | Ki | 0.1090 | 1 | 1 |
| Dihydrofolate reductase | Escherichia coli K-12 | IC50 | 383.5250 | 12 | 12 |
| Dihydrofolate reductase | Homo sapiens (human) | IC50 | 7.6762 | 17 | 17 |
| Dihydrofolate reductase | Lacticaseibacillus casei | IC50 | 173.0750 | 4 | 4 |
| Dihydrofolate reductase | Pneumocystis carinii | IC50 | 230.0000 | 1 | 1 |
| Dihydrofolate reductase | Homo sapiens (human) | Ki | 0.0071 | 3 | 3 |
| Dihydrofolate reductase | Mus musculus (house mouse) | Ki | 0.5600 | 1 | 1 |
| Folate receptor alpha | Homo sapiens (human) | IC50 | 0.2417 | 6 | 6 |
| Folate receptor beta | Homo sapiens (human) | IC50 | 0.2585 | 6 | 6 |
| Proton-coupled folate transporter | Homo sapiens (human) | IC50 | 0.0229 | 5 | 5 |
| Proton-coupled folate transporter | Homo sapiens (human) | Ki | 0.6776 | 7 | 7 |
| Reduced folate transporter | Homo sapiens (human) | IC50 | 0.0928 | 5 | 5 |
| Serine hydroxymethyltransferase, cytosolic | Homo sapiens (human) | Ki | 79.2333 | 3 | 3 |
| Thymidylate synthase | Homo sapiens (human) | IC50 | 15.8118 | 22 | 22 |
| Thymidylate synthase | Lacticaseibacillus casei | IC50 | 29.0000 | 4 | 4 |
| Thymidylate synthase | Homo sapiens (human) | Ki | 0.1142 | 3 | 3 |
| Thymidylate synthase | Lacticaseibacillus casei | Ki | 0.5500 | 1 | 1 |
| Thymidylate synthase | Mus musculus (house mouse) | Ki | 0.3400 | 1 | 1 |
| Thymidylate synthase | Escherichia coli | IC50 | 122.2385 | 13 | 13 |
| Thymidylate synthase | Escherichia coli LF82 | IC50 | 76.0000 | 1 | 1 |
| Thymidylate synthase | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| Trifunctional purine biosynthetic protein adenosine-3 | Homo sapiens (human) | IC50 | 5.0285 | 6 | 6 |
| Trifunctional purine biosynthetic protein adenosine-3 | Mus musculus (house mouse) | IC50 | 20.0000 | 3 | 3 |
| Trifunctional purine biosynthetic protein adenosine-3 | Homo sapiens (human) | Ki | 0.6113 | 4 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Serine hydroxymethyltransferase, cytosolic | Homo sapiens (human) | Kd | 16.9000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Proton-coupled folate transporter | Homo sapiens (human) | K | 0.1570 | 2 | 2 |