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Assay Detail

CHEMBL1101552

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

Binding
Inhibition of Haemophilus influenzae recombinant DapE
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Haemophilus influenzae
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Succinyl-diaminopimelate desuccinylase (CHEMBL1075192)
Type SINGLE PROTEIN
Organism Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)

Publication

Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity.
Gillner D, Armoush N, Holz RC, Becker DP.
Bioorg Med Chem Lett (2009) 19 : 6350 -6352
PubMed 19822427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.56 5.48
Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1560 CAPTOPRIL 4.0 1 5.48
CHEMBL207222 1 4.86
CHEMBL291888 1 4.47
CHEMBL434965 D-CAPTOPRIL 1 4.38
CHEMBL1076479 1 4.37
CHEMBL1430 PENICILLAMINE 4.0 1 4.30
CHEMBL141272 1 4.04
CHEMBL21485 PHENYLBORONIC ACID 1 -
CHEMBL82324 1 -
CHEMBL421765 1 -
CHEMBL31962 BUTYL BORONIC ACID 1 -
CHEMBL578 ENALAPRIL 4.0 1 -
CHEMBL734 ACETOHYDROXAMIC ACID 4.0 1 -
CHEMBL1086896 1 -
CHEMBL263376 PHENYLTHIOUREA 1 -
CHEMBL1088324 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1560 CAPTOPRIL IC50 = 3300.0 nM 5.48
CHEMBL207222 IC50 = 13700.0 nM 4.86
CHEMBL291888 IC50 = 34000.0 nM 4.47
CHEMBL434965 D-CAPTOPRIL IC50 = 42000.0 nM 4.38
CHEMBL1076479 IC50 = 43000.0 nM 4.37
CHEMBL1430 PENICILLAMINE IC50 = 50000.0 nM 4.30
CHEMBL141272 IC50 = 92000.0 nM 4.04
CHEMBL21485 PHENYLBORONIC ACID IC50 = 107000.0 nM -
CHEMBL82324 IC50 > 10000000.0 nM -
CHEMBL421765 IC50 > 10000000.0 nM -
CHEMBL31962 BUTYL BORONIC ACID IC50 ~ 10000000.0 nM -
CHEMBL578 ENALAPRIL IC50 > 1000000.0 nM -
CHEMBL734 ACETOHYDROXAMIC ACID IC50 > 1000000.0 nM -
CHEMBL1086896 IC50 > 1000000.0 nM -
CHEMBL263376 PHENYLTHIOUREA IC50 > 100000.0 nM -
CHEMBL1088324 IC50 = 1620000.0 nM -
CHEMBL1088324 Ki = 800000.0 nM -