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Assay Detail

CHEMBL5229262

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

Binding
Inhibition of human recombinant MMP12 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated with enzyme for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins by fluorescence based analysis
3
Total Activities
3
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

Discovery of Dimeric Arylsulfonamides as Potent ADAM8 Inhibitors.
Cuffaro D, Camodeca C, Tuccinardi T, Ciccone L, Bartsch JW, Kellermann T, Cook L, Nuti E, Rossello A.
ACS Med Chem Lett (2021) 12 : 1787 -1793
PubMed 35111280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.35 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431028 1 8.03
CHEMBL5283335 1 7.39
CHEMBL5267938 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431028 IC50 = 9.4 nM 8.03
CHEMBL5283335 IC50 = 41.0 nM 7.39
CHEMBL5267938 IC50 = 242.0 nM 6.62