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Assay Detail

CHEMBL669444

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

Binding
Inhibition of human WIL2/dihydrofolate reductase activity
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparison of the biological effects of selected 5,8-dideazafolate analogues with their 2-desamino counterparts.
Hynes JB, Patil SA, Hagan RL, Cole A, Kohler W, Freisheim JH.
J Med Chem (1989) 32 : 852 -856
PubMed 2704031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.56 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 8.37
CHEMBL36739 1 6.96
CHEMBL139551 1 6.77
CHEMBL354121 1 6.58
CHEMBL169376 1 6.50
CHEMBL138870 1 6.48
CHEMBL171790 1 6.19
CHEMBL422395 1 6.04
CHEMBL171480 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 4.3 nM 8.37
CHEMBL36739 IC50 = 110.0 nM 6.96
CHEMBL139551 IC50 = 170.0 nM 6.77
CHEMBL354121 IC50 = 260.0 nM 6.58
CHEMBL169376 IC50 = 320.0 nM 6.50
CHEMBL138870 IC50 = 330.0 nM 6.48
CHEMBL171790 IC50 = 650.0 nM 6.19
CHEMBL422395 IC50 = 910.0 nM 6.04
CHEMBL171480 IC50 = 7000.0 nM 5.16