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Assay Detail

CHEMBL667322

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Binding
Evaluated for inhibition of dihydrofolate reductase (DHFR) isolated from L1210 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L1210
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL4564)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.
Piper JR, McCaleb GS, Montgomery JA, Kisliuk RL, Gaumont Y, Thorndike J, Sirotnak FM.
J Med Chem (1988) 31 : 2164 -2169
PubMed 3184124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 10.55 10.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69016 1 10.55
CHEMBL66864 1 -
CHEMBL267890 1 -
CHEMBL34259 METHOTREXATE 4.0 1 -
CHEMBL66389 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69016 Ki = 0.0283 nM 10.55
CHEMBL66864 Ki > 1.0 nM -
CHEMBL267890 Ki > 1.0 nM -
CHEMBL34259 METHOTREXATE Ki = 0.00545 nM -
CHEMBL66389 Ki > 1.0 nM -