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Assay Detail

CHEMBL668775

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Binding
Inhibition of Escherichia coli Dihydrofolate reductase in presence of 100 uM Dihydrofolate reductase
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydrofolate reductase (CHEMBL1809)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.
Zolli-Juran M, Cechetto JD, Hartlen R, Daigle DM, Brown ED.
Bioorg Med Chem Lett (2003) 13 : 2493 -2496
PubMed 12852950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.00 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22 TRIMETHOPRIM 4.0 1 7.43
CHEMBL1160541 1 6.52
CHEMBL82334 1 6.38
CHEMBL310759 2 6.29
CHEMBL85364 1 6.21
CHEMBL83547 1 6.09
CHEMBL84108 1 5.96
CHEMBL82825 1 5.68
CHEMBL309713 1 4.80
CHEMBL82985 1 4.62
CHEMBL80014 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22 TRIMETHOPRIM IC50 = 37.0 nM 7.43
CHEMBL1160541 IC50 = 302.0 nM 6.52
CHEMBL82334 IC50 = 420.0 nM 6.38
CHEMBL310759 IC50 = 510.0 nM 6.29
CHEMBL85364 IC50 = 620.0 nM 6.21
CHEMBL83547 IC50 = 820.0 nM 6.09
CHEMBL310759 IC50 = 1000.0 nM 6.00
CHEMBL84108 IC50 = 1100.0 nM 5.96
CHEMBL82825 IC50 = 2100.0 nM 5.68
CHEMBL309713 IC50 = 16000.0 nM 4.80
CHEMBL82985 IC50 = 24000.0 nM 4.62
CHEMBL80014 IC50 = 120000.0 nM -