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Assay Detail

CHEMBL862516

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Binding
Inhibitory activity against TACE
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Conversion of potent MMP inhibitors into selective TACE inhibitors.
Cherney RJ, King BW, Gilmore JL, Liu RQ, Covington MB, Duan JJ, Decicco CP.
Bioorg Med Chem Lett (2006) 16 : 1028 -1031
PubMed 16289878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.32 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203160 1 8.43
CHEMBL204048 1 8.23
CHEMBL379469 1 8.08
CHEMBL203972 1 6.82
CHEMBL204549 1 6.32
CHEMBL204495 1 6.05
CHEMBL100570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203160 IC50 = 3.7 nM 8.43
CHEMBL204048 IC50 = 5.9 nM 8.23
CHEMBL379469 IC50 = 8.3 nM 8.08
CHEMBL203972 IC50 = 150.0 nM 6.82
CHEMBL204549 IC50 = 480.0 nM 6.32
CHEMBL204495 IC50 = 900.0 nM 6.05
CHEMBL100570 IC50 > 1000.0 nM -