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Assay Detail

CHEMBL664361

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

Binding
Evaluated for the inhibition of chicken liver Dihydrofolate reductase by using standard enzyme assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydrofolate reductase (CHEMBL2575)
Type SINGLE PROTEIN
Organism Gallus gallus

Publication

Lysine and ornithine analogues of methotrexate as inhibitors of dihydrofolate reductase.
Kempton RJ, Black AM, Anstead GM, Kumar AA, Blankenship DT, Freisheim JH.
J Med Chem (1982) 25 : 475 -477
PubMed 7069726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.42 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.05
CHEMBL418165 1 6.89
CHEMBL36083 1 6.60
CHEMBL356340 1 6.48
CHEMBL142626 1 6.42
CHEMBL342744 1 6.02
CHEMBL146440 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 90.0 nM 7.05
CHEMBL418165 IC50 = 130.0 nM 6.89
CHEMBL36083 IC50 = 250.0 nM 6.60
CHEMBL356340 IC50 = 330.0 nM 6.48
CHEMBL142626 IC50 = 380.0 nM 6.42
CHEMBL342744 IC50 = 950.0 nM 6.02
CHEMBL146440 IC50 = 3100.0 nM 5.51