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Assay Detail

CHEMBL663897

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against recombinant lc dihydrofolate reductase(in 50 uM dihydrofolic acid)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Lacticaseibacillus casei
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL2902)
Type SINGLE PROTEIN
Organism Lactobacillus casei

Publication

2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.
Gangjee A, Vasudevan A, Queener SF, Kisliuk RL.
J Med Chem (1996) 39 : 1438 -1446
PubMed 8691474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.90 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.26
CHEMBL33045 1 7.17
CHEMBL33815 1 6.77
CHEMBL32708 1 5.29
CHEMBL32113 1 5.24
CHEMBL33208 1 4.82
CHEMBL32266 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 55.0 nM 7.26
CHEMBL33045 IC50 = 67.0 nM 7.17
CHEMBL33815 IC50 = 170.0 nM 6.77
CHEMBL32708 IC50 = 5100.0 nM 5.29
CHEMBL32113 IC50 = 5700.0 nM 5.24
CHEMBL33208 IC50 = 15000.0 nM 4.82
CHEMBL32266 IC50 = 17000.0 nM 4.77