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Assay Detail

CHEMBL4373201

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

Binding
Inhibition of Escherichia coli C-terminal His6-tagged ClpP expressed Escherichia coli SG1146a using Suc-LY-AMC as substrate preincubated for 10 mins followed by substrate addition and measured over 1 hr by fluorescence assay
106
Total Activities
106
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

ATP-dependent Clp protease proteolytic subunit (CHEMBL3341578)
Type SINGLE PROTEIN
Organism Escherichia coli (strain K12)

Publication

α-Amino Diphenyl Phosphonates as Novel Inhibitors of Escherichia coli ClpP Protease.
Moreno-Cinos C, Sassetti E, Salado IG, Witt G, Benramdane S, Reinhardt L, Cruz CD, Joossens J, Van der Veken P, Brötz-Oesterhelt H, Tammela P, Winterhalter M, Gribbon P, Windshügel B, Augustyns K.
J Med Chem (2019) 62 : 774 -797
PubMed 30571121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 106 5.03 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4551942 1 6.30
CHEMBL4448860 1 6.30
CHEMBL4444802 1 6.22
CHEMBL4483092 1 6.22
CHEMBL4575669 1 5.09
CHEMBL4472140 1 4.88
CHEMBL4446383 1 4.85
CHEMBL4461379 1 4.84
CHEMBL4561263 1 4.42
CHEMBL3770879 1 4.40
CHEMBL4585066 1 4.32
CHEMBL4469279 1 4.30
CHEMBL4442349 1 4.15
CHEMBL4476496 1 4.10
CHEMBL4456475 1 -
CHEMBL4449224 1 -
CHEMBL4435181 1 -
CHEMBL4513583 1 -
CHEMBL4544287 1 -
CHEMBL4544174 1 -
CHEMBL4559730 1 -
CHEMBL4440311 1 -
CHEMBL4440015 1 -
CHEMBL4458565 1 -
CHEMBL4568558 1 -
CHEMBL4444920 1 -
CHEMBL4448396 1 -
CHEMBL4464045 1 -
CHEMBL4437668 1 -
CHEMBL4438438 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448860 IC50 = 500.0 nM 6.30
CHEMBL4551942 IC50 = 500.0 nM 6.30
CHEMBL4483092 IC50 = 600.0 nM 6.22
CHEMBL4444802 IC50 = 600.0 nM 6.22
CHEMBL4575669 IC50 = 8200.0 nM 5.09
CHEMBL4472140 IC50 = 13100.0 nM 4.88
CHEMBL4446383 IC50 = 14200.0 nM 4.85
CHEMBL4461379 IC50 = 14400.0 nM 4.84
CHEMBL4561263 IC50 = 38000.0 nM 4.42
CHEMBL3770879 IC50 = 39800.0 nM 4.40
CHEMBL4585066 IC50 = 48100.0 nM 4.32
CHEMBL4469279 IC50 = 49500.0 nM 4.30
CHEMBL4442349 IC50 = 71300.0 nM 4.15
CHEMBL4476496 IC50 = 79700.0 nM 4.10
CHEMBL4544801 IC50 - -
CHEMBL4517157 IC50 - -
CHEMBL4452077 IC50 - -
CHEMBL4451640 IC50 - -
CHEMBL4476717 IC50 - -
CHEMBL4462723 IC50 - -
CHEMBL4438501 IC50 - -
CHEMBL4449129 IC50 - -
CHEMBL4593483 IC50 - -
CHEMBL4532659 IC50 - -
CHEMBL4513936 IC50 - -
CHEMBL4460911 IC50 - -
CHEMBL4587430 IC50 - -
CHEMBL4546615 IC50 - -
CHEMBL4466511 IC50 - -
CHEMBL4532734 IC50 - -
CHEMBL4545719 IC50 - -
CHEMBL4519525 IC50 - -
CHEMBL4563688 IC50 - -
CHEMBL393591 IC50 - -
CHEMBL4436632 IC50 - -
CHEMBL4442639 IC50 - -
CHEMBL4550461 IC50 - -
CHEMBL4524547 IC50 - -
CHEMBL4559386 IC50 - -
CHEMBL4540480 IC50 - -
CHEMBL4516940 IC50 - -
CHEMBL4527515 IC50 - -
CHEMBL4551194 IC50 - -
CHEMBL4560967 IC50 - -
CHEMBL4475830 IC50 - -
CHEMBL4522091 IC50 - -
CHEMBL4544896 IC50 - -
CHEMBL4585121 IC50 - -
CHEMBL4519292 IC50 - -
CHEMBL4475828 IC50 - -