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Assay Detail

CHEMBL1681028

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of trimethoprim-resistant Staphylococcus aureus Type S1 dihydrofolate reductase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

In vitro and in vivo properties of dihydrophthalazine antifolates, a novel family of antibacterial drugs.
Caspers P, Bury L, Gaucher B, Heim J, Shapiro S, Siegrist S, Schmitt-Hoffmann A, Thenoz L, Urwyler H.
Antimicrob Agents Chemother (2009) 53 : 3620 -3627
PubMed 19546364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.35 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1673175 1 7.46
CHEMBL1673173 1 7.01
CHEMBL1673177 1 7.01
CHEMBL1650306 1 6.92
CHEMBL1650308 1 6.81
CHEMBL1673176 1 6.00
CHEMBL1673174 1 5.88
CHEMBL1673178 1 5.59
CHEMBL22 TRIMETHOPRIM 4.0 1 4.48
CHEMBL1650307 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1673175 IC50 = 35.1 nM 7.46
CHEMBL1673173 IC50 = 98.3 nM 7.01
CHEMBL1673177 IC50 = 98.0 nM 7.01
CHEMBL1650306 IC50 = 121.1 nM 6.92
CHEMBL1650308 IC50 = 153.6 nM 6.81
CHEMBL1673176 IC50 = 1009.0 nM 6.00
CHEMBL1673174 IC50 = 1327.0 nM 5.88
CHEMBL1673178 IC50 = 2586.0 nM 5.59
CHEMBL22 TRIMETHOPRIM IC50 = 32997.0 nM 4.48
CHEMBL1650307 IC50 - -