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Assay Detail

CHEMBL995078

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

Binding
Inhibition of human dihydrofolate reductase by spectrophotometry
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium.
Bolstad DB, Bolstad ES, Frey KM, Wright DL, Anderson AC.
J Med Chem (2008) 51 : 6839 -6852
PubMed 18834108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.68 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457725 1 5.90
CHEMBL485569 1 5.87
CHEMBL459177 1 5.87
CHEMBL223301 1 5.86
CHEMBL459178 1 5.86
CHEMBL457905 1 5.85
CHEMBL520358 1 5.77
CHEMBL457906 1 5.56
CHEMBL458817 1 5.47
CHEMBL458829 1 5.38
CHEMBL457726 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457725 IC50 = 1250.0 nM 5.90
CHEMBL485569 IC50 = 1360.0 nM 5.87
CHEMBL459177 IC50 = 1360.0 nM 5.87
CHEMBL223301 IC50 = 1380.0 nM 5.86
CHEMBL459178 IC50 = 1380.0 nM 5.86
CHEMBL457905 IC50 = 1420.0 nM 5.85
CHEMBL520358 IC50 = 1700.0 nM 5.77
CHEMBL457906 IC50 = 2770.0 nM 5.56
CHEMBL458817 IC50 = 3370.0 nM 5.47
CHEMBL458829 IC50 = 4200.0 nM 5.38
CHEMBL457726 IC50 = 7200.0 nM 5.14