Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL668783

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

Binding
Inhibitory activity against purified dihydrofolate reductase from rat
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities.
Gangjee A, Zaveri N, Kothare M, Queener SF.
J Med Chem (1995) 38 : 3660 -3668
PubMed 7658454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.95 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119 TRIMETREXATE 4.0 1 8.52
CHEMBL121433 1 7.47
CHEMBL123122 1 7.42
CHEMBL121348 1 7.33
CHEMBL123043 1 7.17
CHEMBL121683 1 7.15
CHEMBL120821 1 7.13
CHEMBL264548 1 6.94
CHEMBL120994 1 6.82
CHEMBL123276 1 6.64
CHEMBL121868 1 6.58
CHEMBL7263 1 6.25
CHEMBL420332 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119 TRIMETREXATE IC50 = 3.0 nM 8.52
CHEMBL121433 IC50 = 34.0 nM 7.47
CHEMBL123122 IC50 = 38.0 nM 7.42
CHEMBL121348 IC50 = 47.0 nM 7.33
CHEMBL123043 IC50 = 67.0 nM 7.17
CHEMBL121683 IC50 = 71.0 nM 7.15
CHEMBL120821 IC50 = 74.0 nM 7.13
CHEMBL264548 IC50 = 116.0 nM 6.94
CHEMBL120994 IC50 = 150.0 nM 6.82
CHEMBL123276 IC50 = 227.0 nM 6.64
CHEMBL121868 IC50 = 260.0 nM 6.58
CHEMBL7263 IC50 = 560.0 nM 6.25
CHEMBL420332 IC50 = 12700.0 nM 4.90