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Assay Detail

CHEMBL668118

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Binding
Inhibitory activity against Dihydrofolate reductase of Escherichia coli
41
Total Activities
41
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

2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 5. 3',5'-Dimethoxy-4'-substituted-benzyl analogues of trimethoprim.
Roth B, Aig E, Rauckman BS, Strelitz JZ, Phillips AP, Ferone R, Bushby SR, Sigel CW.
J Med Chem (1981) 24 : 933 -941
PubMed 7035668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 7.82 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171639 1 8.40
CHEMBL56282 1 8.40
CHEMBL369211 1 8.38
CHEMBL172805 1 8.38
CHEMBL176489 1 8.30
CHEMBL22 TRIMETHOPRIM 4.0 1 8.30
CHEMBL427305 1 8.28
CHEMBL423434 1 8.20
CHEMBL263732 1 8.13
CHEMBL367061 1 8.11
CHEMBL173641 1 8.10
CHEMBL173901 1 8.00
CHEMBL174433 1 8.00
CHEMBL1181 4-HYDROXYTRIMETHOPRIM 1 7.96
CHEMBL170369 1 7.89
CHEMBL173175 1 7.85
CHEMBL366561 1 7.85
CHEMBL173265 1 7.85
CHEMBL279509 1 7.85
CHEMBL367218 1 7.82
CHEMBL369057 1 7.82
CHEMBL174309 1 7.82
CHEMBL172495 1 7.80
CHEMBL322001 1 7.77
CHEMBL32039 TETROXOPRIM 2.0 1 7.75
CHEMBL366869 1 7.75
CHEMBL173069 1 7.75
CHEMBL105006 1 7.70
CHEMBL174091 1 7.70
CHEMBL174404 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171639 IC50 = 4.0 nM 8.40
CHEMBL56282 IC50 = 4.0 nM 8.40
CHEMBL172805 IC50 = 4.2 nM 8.38
CHEMBL369211 IC50 = 4.2 nM 8.38
CHEMBL176489 IC50 = 5.0 nM 8.30
CHEMBL22 TRIMETHOPRIM IC50 = 5.0 nM 8.30
CHEMBL427305 IC50 = 5.2 nM 8.28
CHEMBL423434 IC50 = 6.3 nM 8.20
CHEMBL263732 IC50 = 7.4 nM 8.13
CHEMBL367061 IC50 = 7.8 nM 8.11
CHEMBL173641 IC50 = 8.0 nM 8.10
CHEMBL173901 IC50 = 10.0 nM 8.00
CHEMBL174433 IC50 = 9.9 nM 8.00
CHEMBL1181 4-HYDROXYTRIMETHOPRIM IC50 = 11.0 nM 7.96
CHEMBL170369 IC50 = 13.0 nM 7.89
CHEMBL173175 IC50 = 14.0 nM 7.85
CHEMBL279509 IC50 = 14.0 nM 7.85
CHEMBL173265 IC50 = 14.0 nM 7.85
CHEMBL366561 IC50 = 14.0 nM 7.85
CHEMBL174309 IC50 = 15.0 nM 7.82
CHEMBL369057 IC50 = 15.0 nM 7.82
CHEMBL367218 IC50 = 15.0 nM 7.82
CHEMBL172495 IC50 = 16.0 nM 7.80
CHEMBL322001 IC50 = 17.0 nM 7.77
CHEMBL32039 TETROXOPRIM IC50 = 18.0 nM 7.75
CHEMBL366869 IC50 = 18.0 nM 7.75
CHEMBL173069 IC50 = 18.0 nM 7.75
CHEMBL105006 IC50 = 20.0 nM 7.70
CHEMBL174091 IC50 = 20.0 nM 7.70
CHEMBL174404 IC50 = 20.0 nM 7.70
CHEMBL173595 IC50 = 21.0 nM 7.68
CHEMBL173709 IC50 = 22.0 nM 7.66
CHEMBL171839 IC50 = 22.0 nM 7.66
CHEMBL355793 IC50 = 24.0 nM 7.62
CHEMBL172808 IC50 = 28.0 nM 7.55
CHEMBL174033 IC50 = 40.0 nM 7.40
CHEMBL368393 IC50 = 46.0 nM 7.34
CHEMBL172131 IC50 = 46.0 nM 7.34
CHEMBL287241 IC50 = 56.0 nM 7.25
CHEMBL318078 IC50 = 62.0 nM 7.21
CHEMBL104675 IC50 = 320.0 nM 6.50