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Assay Detail

CHEMBL3635313

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Binding
Inhibition of Escherichia coli DHFR assessed as NADP formation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL1809)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase.
Srinivasan B, Tonddast-Navaei S, Skolnick J.
Eur J Med Chem (2015) 103 : 600 -614
PubMed 26414808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.85 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97313 1 5.94
CHEMBL97567 1 5.74
CHEMBL94742 1 5.12
CHEMBL1617293 1 4.73
CHEMBL268914 1 4.70
CHEMBL747 CYCLOGUANIL 2.0 1 4.68
CHEMBL548155 1 4.49
CHEMBL316611 1 4.20
CHEMBL266573 1 4.05
CHEMBL97830 1 -
CHEMBL589682 1 -
CHEMBL333873 1 -
CHEMBL1625056 1 -
CHEMBL3634634 1 -
CHEMBL1412044 1 -
CHEMBL741 LAMOTRIGINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97313 IC50 = 1150.0 nM 5.94
CHEMBL97567 IC50 = 1840.0 nM 5.74
CHEMBL94742 IC50 = 7590.0 nM 5.12
CHEMBL1617293 IC50 = 18450.0 nM 4.73
CHEMBL268914 IC50 = 20190.0 nM 4.70
CHEMBL747 CYCLOGUANIL IC50 = 20910.0 nM 4.68
CHEMBL548155 IC50 = 32270.0 nM 4.49
CHEMBL316611 IC50 = 62830.0 nM 4.20
CHEMBL266573 IC50 = 89100.0 nM 4.05
CHEMBL97830 IC50 - -
CHEMBL589682 IC50 - -
CHEMBL333873 IC50 = 262700.0 nM -
CHEMBL1625056 IC50 = 478400.0 nM -
CHEMBL3634634 IC50 = 721600.0 nM -
CHEMBL1412044 IC50 = 1548000.0 nM -
CHEMBL741 LAMOTRIGINE IC50 = 348900.0 nM -