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Assay Detail

CHEMBL3134686

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

Binding
Inhibition of human recombinant MMP12 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 10 mins prior to substrate addition by spectrophotometry
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Macrophage metalloelastase (CHEMBL4393)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The advantage of biosensor analysis over enzyme inhibition studies for slow dissociating inhibitors characterization of hydroxamate-based matrix metalloproteinase-12 inhibitors
Gossas T, Nordstrom H, Xu M, Sun Z, Lin G, Wallberg H, Danielson UH
Medchemcomm (2013) 4 : 432 -442
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.20 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3133269 1 9.00
CHEMBL115727 1 8.72
CHEMBL19611 ILOMASTAT 2.0 1 8.42
CHEMBL3133267 1 7.52
CHEMBL3133268 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3133269 Ki = 1.0 nM 9.00
CHEMBL115727 Ki = 1.9 nM 8.72
CHEMBL19611 ILOMASTAT Ki = 3.8 nM 8.42
CHEMBL3133267 Ki = 30.0 nM 7.52
CHEMBL3133268 Ki = 48.0 nM 7.32