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ChEMBL

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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL202
Target Type SINGLE PROTEIN
Preferred Name Dihydrofolate reductase
Synonyms DHFR | Dihydrofolate reductase
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > oxidoreductase

Target Components

Component Description Relationship Accession
Dihydrofolate reductase SINGLE PROTEIN P00374

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL34259 METHOTREXATE Dihydrofolate reductase inhibitor 4 DailyMed
CHEMBL1201746 PRALATREXATE Dihydrofolate reductase inhibitor 4 DailyMed
CHEMBL2360464 PEMETREXED DISODIUM Dihydrofolate reductase inhibitor 4 DailyMed
CHEMBL3244648 METHOTREXATE SODIUM Dihydrofolate reductase inhibitor 4 DailyMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000228716
Ensembl ENSG00000228716
GO Cellular Component GO:0005575 (cellular_component)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005829 (cytosol)
GO Molecular Function GO:0000900 (translation repressor activity, nucleic acid binding)
GO:0003723 (RNA binding)
GO:0003729 (mRNA binding)
GO:0004146 (dihydrofolate reductase activity)
GO:0005542 (folic acid binding)
GO:0008144 (drug binding)
GO:0016491 (oxidoreductase activity)
GO:0033560 (folate reductase activity)
GO:0051870 (methotrexate binding)
GO:0070402 (NADPH binding)
GO:1990825 (sequence-specific mRNA binding)
GO Biological Process GO:0000083 (regulation of transcription involved in G1/S transition of mitotic cell cycle)
GO:0006729 (tetrahydrobiopterin biosynthetic process)
GO:0006730 (one-carbon metabolic process)
GO:0017148 (negative regulation of translation)
GO:0031103 (axon regeneration)
GO:0031427 (response to methotrexate)
GO:0046452 (dihydrofolate metabolic process)
GO:0046653 (tetrahydrofolate metabolic process)
GO:0046654 (tetrahydrofolate biosynthetic process)
GO:0046655 (folic acid metabolic process)
GO:0051000 (positive regulation of nitric-oxide synthase activity)
GO:0055114 (oxidation-reduction process)
GO:2000121 (regulation of removal of superoxide radicals)
Wikipedia Dihydrofolate_reductase

Target Cross References - Protein

canSAR P00374
CGD Megablastic anemia due to dihydrofolate reductase deficiency
Human Protein Atlas ENSG00000228716
IntAct P00374
Guide to Pharmacology 2603
Open Targets ENSG00000228716
PharmGKB PA143
Reactome R-HSA-1474151 (Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation.)
R-HSA-196757 (Metabolism of folate and pterines.)
R-HSA-539107 (Activation of E2F1 target genes at G1/S.)
UniProt B4DDD2 P00374 Q14130 Q6IRW8

Target Cross References - Domain

InterPro IPR001796 (DHFR_dom.)
IPR012259 (DHFR.)
IPR017925 (DHFR_CS.)
IPR024072 (DHFR-like_dom_sf.)
Pfam PF00186 (DHFR_1)

Target Cross References - Structure

PDBe 1BOZ 1DHF 1DLR 1DLS 1DRF 1HFP 1HFQ 1HFR 1KMS 1KMV 1MVS 1MVT 1OHJ 1OHK 1PD8 1PD9 1PDB 1S3U 1S3V 1S3W 1U71 1U72 2C2S 2C2T More...
CREDO 1BOZ 1DHF 1DLR 1DLS 1DRF 1HFP 1HFQ 1HFR 1KMS 1KMV 1MVS 1MVT 1OHJ 1OHK 1PD8 1PD9 1PDB 1S3U 1S3V 1S3W 1U71 1U72 2C2S 2C2T More...
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