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Assay Detail

CHEMBL664461

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

Binding
Inhibitory activity against dihydropteroic acid synthase (SYN) from Escherichia coli
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.
Otzen T, Wempe EG, Kunz B, Bartels R, Lehwark-Yvetot G, Hänsel W, Schaper KJ, Seydel JK.
J Med Chem (2004) 47 : 240 -253
PubMed 14695838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.30 4.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143174 1 4.46
CHEMBL1043 DAPSONE 4.0 1 4.46
CHEMBL48396 ACEDIASULFONE 2.0 1 4.43
CHEMBL358252 1 4.38
CHEMBL353260 1 4.33
CHEMBL143106 1 4.13
CHEMBL1246 MONO-N-ACETYL DAPSONE 1 4.12
CHEMBL142844 1 4.05
CHEMBL357499 1 -
CHEMBL172231 1 -
CHEMBL143754 1 -
CHEMBL352594 1 -
CHEMBL140585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143174 IC50 = 34920.0 nM 4.46
CHEMBL1043 DAPSONE IC50 = 34360.0 nM 4.46
CHEMBL48396 ACEDIASULFONE IC50 = 37050.0 nM 4.43
CHEMBL358252 IC50 = 41710.0 nM 4.38
CHEMBL353260 IC50 = 46210.0 nM 4.33
CHEMBL143106 IC50 = 74240.0 nM 4.13
CHEMBL1246 MONO-N-ACETYL DAPSONE IC50 = 75650.0 nM 4.12
CHEMBL142844 IC50 = 89850.0 nM 4.05
CHEMBL357499 IC50 = 116000.0 nM -
CHEMBL172231 IC50 = 155390.0 nM -
CHEMBL143754 IC50 = 128200.0 nM -
CHEMBL352594 IC50 = 101240.0 nM -
CHEMBL140585 IC50 = 149000.0 nM -