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Assay Detail

CHEMBL2434050

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

Binding
Inhibition of ADAM-17 in human A2780 cells assessed as inhibition of EGF-induced sALCAM release incubated for 30 mins prior to EGF induction measured after 18 hrs by ELISA
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models.
Nuti E, Casalini F, Santamaria S, Fabbi M, Carbotti G, Ferrini S, Marinelli L, La Pietra V, Novellino E, Camodeca C, Orlandini E, Nencetti S, Rossello A.
J Med Chem (2013) 56 : 8089 -8103
PubMed 24044434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.64 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431028 1 6.07
CHEMBL1089842 1 5.84
CHEMBL2431027 1 5.00
CHEMBL2431026 1 -
CHEMBL2431021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431028 IC50 = 845.0 nM 6.07
CHEMBL1089842 IC50 = 1436.0 nM 5.84
CHEMBL2431027 IC50 = 10000.0 nM 5.00
CHEMBL2431026 IC50 > 10000.0 nM -
CHEMBL2431021 IC50 > 10000.0 nM -