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Assay Detail

CHEMBL5229258

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

Binding
Inhibition of recombinant ADAM17 (unknown origin) using PepDAB13 as substrate preincubated with enzyme for 45 mins followed by substrate addition and measured for 6 hrs by fluorometric assay
4
Total Activities
4
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

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 4 7.72 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431028 1 8.72
CHEMBL5283335 1 7.62
CHEMBL5267938 1 7.28
CHEMBL5276957 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431028 IC50 = 1.9 nM 8.72
CHEMBL5283335 IC50 = 24.0 nM 7.62
CHEMBL5267938 IC50 = 52.0 nM 7.28
CHEMBL5276957 IC50 = 55.0 nM 7.26