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Assay Detail

CHEMBL664866

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Binding
Inhibition constant against Dihydrofolate reductase
11
Total Activities
10
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
Ki 11 6.70 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22 TRIMETHOPRIM 4.0 1 8.42
CHEMBL1160541 1 7.58
CHEMBL82334 1 7.39
CHEMBL310759 2 7.21
CHEMBL85364 1 7.19
CHEMBL84108 1 6.89
CHEMBL82825 1 6.72
CHEMBL309713 1 5.70
CHEMBL80014 1 4.96
CHEMBL82985 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22 TRIMETHOPRIM Ki = 3.8 nM 8.42
CHEMBL1160541 Ki = 26.0 nM 7.58
CHEMBL82334 Ki = 41.0 nM 7.39
CHEMBL310759 Ki = 61.0 nM 7.21
CHEMBL85364 Ki = 65.0 nM 7.19
CHEMBL310759 Ki = 93.0 nM 7.03
CHEMBL84108 Ki = 130.0 nM 6.89
CHEMBL82825 Ki = 190.0 nM 6.72
CHEMBL309713 Ki = 2000.0 nM 5.70
CHEMBL80014 Ki = 11000.0 nM 4.96
CHEMBL82985 Ki = 23000.0 nM 4.64