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Assay Detail

CHEMBL681438

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Binding
Inhibition of GAR transformylase from mammalian L1210 cells
3
Total Activities
3
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

Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3690)
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
IC50 3 5.20 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267890 1 6.30
CHEMBL66389 1 4.10
CHEMBL66864 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267890 IC50 = 500.0 nM 6.30
CHEMBL66389 IC50 = 80000.0 nM 4.10
CHEMBL66864 IC50 > 20000.0 nM -