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Assay Detail

CHEMBL887626

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Binding
Inhibition of pTACE
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Publication

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Sheppeck JE, Gilmore JL, Tebben A, Xue CB, Liu RQ, Decicco CP, Duan JJ.
Bioorg Med Chem Lett (2007) 17 : 2769 -2774
PubMed 17368021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148169 1 9.00
CHEMBL228320 1 8.05
CHEMBL229072 1 7.85
CHEMBL229070 1 7.54
CHEMBL228318 1 7.47
CHEMBL388124 1 7.43
CHEMBL389691 1 6.79
CHEMBL228268 1 6.36
CHEMBL228319 1 5.80
CHEMBL228267 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148169 IC50 = 1.0 nM 9.00
CHEMBL228320 IC50 = 9.0 nM 8.05
CHEMBL229072 IC50 = 14.0 nM 7.85
CHEMBL229070 IC50 = 29.0 nM 7.54
CHEMBL228318 IC50 = 34.0 nM 7.47
CHEMBL388124 IC50 = 37.0 nM 7.43
CHEMBL389691 IC50 = 162.0 nM 6.79
CHEMBL228268 IC50 = 439.0 nM 6.36
CHEMBL228319 IC50 = 1600.0 nM 5.80
CHEMBL228267 IC50 > 1000.0 nM -