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Assay Detail

CHEMBL885870

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Binding
Inhibition of porcine TACE
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Sheppeck JE, Gilmore JL, Yang A, Chen XT, Xue CB, Roderick J, Liu RQ, Covington MB, Decicco CP, Duan JJ.
Bioorg Med Chem Lett (2007) 17 : 1413 -1417
PubMed 17188863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.92 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246577 2 7.96
CHEMBL245581 1 7.89
CHEMBL245384 1 7.62
CHEMBL429107 1 7.62
CHEMBL245582 1 7.60
CHEMBL442421 1 7.55
CHEMBL229070 1 7.54
CHEMBL245383 1 7.27
CHEMBL246376 1 7.19
CHEMBL392172 1 7.01
CHEMBL393863 1 6.82
CHEMBL246563 1 6.77
CHEMBL245774 1 6.68
CHEMBL393444 1 6.64
CHEMBL245382 1 6.57
CHEMBL393445 1 6.05
CHEMBL245776 1 5.43
CHEMBL391362 1 5.26
CHEMBL246576 1 5.13
CHEMBL246171 1 -
CHEMBL245974 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246577 IC50 = 11.0 nM 7.96
CHEMBL245581 IC50 = 13.0 nM 7.89
CHEMBL246577 IC50 = 17.0 nM 7.77
CHEMBL245384 IC50 = 24.0 nM 7.62
CHEMBL429107 IC50 = 24.0 nM 7.62
CHEMBL245582 IC50 = 25.0 nM 7.60
CHEMBL442421 IC50 = 28.0 nM 7.55
CHEMBL229070 IC50 = 29.0 nM 7.54
CHEMBL245383 IC50 = 54.0 nM 7.27
CHEMBL246376 IC50 = 64.0 nM 7.19
CHEMBL392172 IC50 = 98.0 nM 7.01
CHEMBL393863 IC50 = 150.0 nM 6.82
CHEMBL246563 IC50 = 170.0 nM 6.77
CHEMBL245774 IC50 = 210.0 nM 6.68
CHEMBL393444 IC50 = 230.0 nM 6.64
CHEMBL245382 IC50 = 270.0 nM 6.57
CHEMBL393445 IC50 = 900.0 nM 6.05
CHEMBL245776 IC50 = 3700.0 nM 5.43
CHEMBL391362 IC50 = 5500.0 nM 5.26
CHEMBL246576 IC50 = 7400.0 nM 5.13
CHEMBL246171 IC50 > 100000.0 nM -
CHEMBL245974 IC50 > 100000.0 nM -