methotrexate
An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.
Ligand Summary
UNII: YL5FZ2Y5U1
PubChem: 126941
Guide to Pharmacology: 4815
ChEMBL: CHEMBL34259
DrugCentral: 1751
LyCHI: QBHCSP2DG8TT
Target Activities
DHFR
Dihydrofolate reductase
80 Activities
Items per page:
1 – 10 of 80
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.92 | |||||
Ki | 11 | Eur J Med Chem, (2017) 135:None:467 | ||||
Ki | 10.42 | Bioorg. Med. Chem. Lett., (1999) 9:10:1463 | ||||
Ki | 10.11 | Bioorg. Med. Chem., (2009) 17:20:7324 | ||||
Ki | 9.96 | J. Med. Chem., (1995) 38:5:745 | ||||
Ki | 9.75 | Bioorg. Med. Chem. Lett., (1999) 9:10:1463 | ||||
IC50 | 9.22 | J. Med. Chem., (1996) 39:1:56 | ||||
IC50 | 9.15 | J. Med. Chem., (1995) 38:19:3798 | ||||
IC50 | 9.14 | J. Med. Chem., (1996) 39:1:56 | ||||
IC50 | 9.09 | J. Med. Chem., (1996) 39:13:2536 | ||||
FOLR1
Folate receptor alpha
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.94 | J. Med. Chem., (2014) 57:19:8152 | ||||
IC50 | 6.94 | J Med Chem, (2018) 61:5:2027 | ||||
IC50 | 6.67 | J Med Chem, (2018) 61:5:2027 | ||||
IC50 | 6.34 | J. Med. Chem., (2014) 57:19:8152 | ||||
IC50 | 6.94 | |||||
FOLR2
Folate receptor beta
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.97 | J. Med. Chem., (2014) 57:19:8152 | ||||
IC50 | 6.97 | J Med Chem, (2018) 61:5:2027 | ||||
IC50 | 6.68 | J. Med. Chem., (2014) 57:19:8152 | ||||
IC50 | 6.68 | J Med Chem, (2018) 61:5:2027 | ||||
IC50 | 6.97 | |||||
SLC19A1
Folate transporter 1
3 Activities
SLC46A1
Proton-coupled folate transporter
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.92 | J. Med. Chem., (2014) 57:19:8152 | ||||
IC50 | 6.92 | J Med Chem, (2018) 61:5:2027 | ||||
IC50 | 6.92 | |||||
HMGB1
High mobility group protein B1
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.62 | J Med Chem, (2018) 61:12:5093 | ||||
Kd | 6.3 | J Med Chem, (2018) 61:12:5093 | ||||
Kd | 7.62 | |||||
TYMS
Thymidylate synthase
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.22 | J. Med. Chem., (2012) 55:19:8318 | ||||
NCOA3
Nuclear receptor coactivator 3
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.68 | None, None:None:None | ||||