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Assay Detail

CHEMBL4621228

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

Binding
Inhibition of Clostridium histolyticum ColH peptidase domain expressed in Escherichia coli BL21(DE3) cells using Mca-Ala-Gly-Pro-Pro-Gly-Pro-Dpa-Gly-Arg-NH2 as substrate preincubated for 1 hr followed by substrate addition measured for 2 mins by FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hathewaya histolytica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Collagenase ColH (CHEMBL4630869)
Type SINGLE PROTEIN
Organism Hathewaya histolytica

Publication

<i>N</i>-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting <i>Pseudomonas aeruginosa</i> Elastase and <i>Clostridium</i> Collagenases.
Konstantinović J, Yahiaoui S, Alhayek A, Haupenthal J, Schönauer E, Andreas A, Kany AM, Müller R, Koehnke J, Berger FK, Bischoff M, Hartmann RW, Brandstetter H, Hirsch AKH.
J Med Chem (2020) 63 : 8359 -8368
PubMed 32470298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.16 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4640494 1 7.77
CHEMBL4636059 1 7.22
CHEMBL4637937 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4640494 IC50 = 17.0 nM 7.77
CHEMBL4636059 IC50 = 60.0 nM 7.22
CHEMBL4637937 IC50 = 320.0 nM 6.50