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Assay Detail

CHEMBL664885

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Binding
Inhibitory activity against Escherichia coli dihydrofolate reductase
11
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 Expert

Target

Dihydrofolate reductase type 1 (CHEMBL2627)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

On the optimization of hydrophobic and hydrophilic substituent interactions of 2,4-diamino-5-(substituted-benzyl)pyrimidines with dihydrofolate reductase.
Selassie CD, Li RL, Poe M, Hansch C.
J Med Chem (1991) 34 : 46 -54
PubMed 1899453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.19 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57343 1 8.02
CHEMBL57383 1 7.94
CHEMBL300114 1 7.80
CHEMBL280378 EPIROPRIM 2.0 1 7.66
CHEMBL21395 1 7.35
CHEMBL56129 1 7.13
CHEMBL434787 1 6.92
CHEMBL56146 1 6.89
CHEMBL298955 1 6.60
CHEMBL31055 1 6.57
CHEMBL19414 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57343 Ki = 9.55 nM 8.02
CHEMBL57383 Ki = 11.48 nM 7.94
CHEMBL300114 Ki = 15.85 nM 7.80
CHEMBL280378 EPIROPRIM Ki = 21.88 nM 7.66
CHEMBL21395 Ki = 44.67 nM 7.35
CHEMBL56129 Ki = 74.13 nM 7.13
CHEMBL434787 Ki = 120.23 nM 6.92
CHEMBL56146 Ki = 128.82 nM 6.89
CHEMBL298955 Ki = 251.19 nM 6.60
CHEMBL31055 Ki = 269.15 nM 6.57
CHEMBL19414 Ki = 630.96 nM 6.20