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Assay Detail

CHEMBL668082

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

Binding
Inhibitory concentration against CCRF-CEM leukemic cell DHFR(Dihydro folate reductase).
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CCRF-CEM
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.
Gangjee A, Devraj R, McGuire JJ, Kisliuk RL.
J Med Chem (1995) 38 : 3798 -3805
PubMed 7562910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.76 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 9.15
CHEMBL323565 1 6.60
CHEMBL106699 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 0.7 nM 9.15
CHEMBL323565 IC50 = 250.0 nM 6.60
CHEMBL106699 IC50 = 30500.0 nM 4.52