Pharos : Ligand Details - methotrexate

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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

Ligand Structure

chemical structure image

Synonyms & Links

UNII: YL5FZ2Y5U1

PubChem: 126941

Guide to Pharmacology: 4815

ChEMBL: CHEMBL426

ChEMBL: CHEMBL34259

DrugCentral: 1751

LyCHI: QBHCSP2DG8TT

Target Activities

DHFR

Tclin

Dihydrofolate reductase

66 Activities

Items per page:

1 – 10 of 66

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.14		J. Med. Chem., (1996) 39:1:66	8568828

IC50	7.1		Bioorg. Med. Chem., (2010) 18:8:2849	20350811

IC50	7.18		J. Med. Chem., (2001) 44:12:1993	11384244

IC50	7.4		J. Med. Chem., (1995) 38:19:3798	7562910

IC50	7.42		J. Med. Chem., (1996) 39:7:1438	8691474

IC50	7.46		Bioorg. Med. Chem., (2007) 15:3:1266	17127067

IC50	7.48		Eur. J. Med. Chem., (2009) 44:2:764	18555562

IC50	7.52		J. Med. Chem., (1990) 33:1:212	2296020

IC50	7.58		J. Med. Chem., (1980) 23:3:320	7365749

IC50	7.6		J. Med. Chem., (1991) 34:1:203	1992118

FOLR2

Tchem

Folate receptor beta

3 Activities

Items per page:

1 – 3 of 3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.68		J. Med. Chem., (2014) 57:19:8152	25234128

IC50	6.97		J. Med. Chem., (2014) 57:19:8152	25234128

IC50	6.96999979		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL426

FOLR1

Tchem

Folate receptor alpha

3 Activities

Items per page:

1 – 3 of 3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.34		J. Med. Chem., (2014) 57:19:8152	25234128

IC50	6.94		J. Med. Chem., (2014) 57:19:8152	25234128

IC50	6.94000006		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL426

SLC19A1

Tchem

Folate transporter 1

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.92		J. Med. Chem., (2014) 57:19:8152	25234128

Ki	5.32999992			15615544

SLC46A1

Tchem

Proton-coupled folate transporter

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.92		J. Med. Chem., (2014) 57:19:8152	25234128

IC50	6.92000008		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL426

TYMS

Tclin

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	22946585