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Assay Detail

CHEMBL902114

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Binding
Inhibition of porcine TACE
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Duan JJ, Chen L, Lu Z, Jiang B, Asakawa N, Sheppeck JE, Liu RQ, Covington MB, Pitts W, Kim SH, Decicco CP.
Bioorg Med Chem Lett (2007) 17 : 266 -271
PubMed 17027261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.09 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395880 1 8.70
CHEMBL247966 1 8.30
CHEMBL241051 1 8.15
CHEMBL240855 1 8.00
CHEMBL427861 1 7.89
CHEMBL395878 1 7.89
CHEMBL240854 1 7.85
CHEMBL240464 1 7.80
CHEMBL440048 1 7.75
CHEMBL240653 1 7.72
CHEMBL247967 1 7.62
CHEMBL241048 1 7.58
CHEMBL240465 1 7.54
CHEMBL391288 1 7.54
CHEMBL395877 1 7.54
CHEMBL240648 1 7.51
CHEMBL429112 1 7.44
CHEMBL248172 1 7.36
CHEMBL240652 1 7.33
CHEMBL438125 1 7.28
CHEMBL240654 1 7.26
CHEMBL248173 1 7.26
CHEMBL428212 1 7.24
CHEMBL240852 1 7.24
CHEMBL393944 1 7.21
CHEMBL392867 1 6.96
CHEMBL391376 1 6.89
CHEMBL442423 1 6.86
CHEMBL241047 1 6.10
CHEMBL193316 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395880 IC50 = 2.0 nM 8.70
CHEMBL247966 IC50 = 5.0 nM 8.30
CHEMBL241051 IC50 = 7.0 nM 8.15
CHEMBL240855 IC50 = 10.0 nM 8.00
CHEMBL427861 IC50 = 13.0 nM 7.89
CHEMBL395878 IC50 = 13.0 nM 7.89
CHEMBL240854 IC50 = 14.0 nM 7.85
CHEMBL240464 IC50 = 16.0 nM 7.80
CHEMBL440048 IC50 = 18.0 nM 7.75
CHEMBL240653 IC50 = 19.0 nM 7.72
CHEMBL247967 IC50 = 24.0 nM 7.62
CHEMBL241048 IC50 = 26.0 nM 7.58
CHEMBL240465 IC50 = 29.0 nM 7.54
CHEMBL391288 IC50 = 29.0 nM 7.54
CHEMBL395877 IC50 = 29.0 nM 7.54
CHEMBL240648 IC50 = 31.0 nM 7.51
CHEMBL429112 IC50 = 36.0 nM 7.44
CHEMBL248172 IC50 = 44.0 nM 7.36
CHEMBL240652 IC50 = 47.0 nM 7.33
CHEMBL438125 IC50 = 52.0 nM 7.28
CHEMBL248173 IC50 = 55.0 nM 7.26
CHEMBL240654 IC50 = 55.0 nM 7.26
CHEMBL428212 IC50 = 58.0 nM 7.24
CHEMBL240852 IC50 = 57.0 nM 7.24
CHEMBL393944 IC50 = 62.0 nM 7.21
CHEMBL392867 IC50 = 111.0 nM 6.96
CHEMBL391376 IC50 = 128.0 nM 6.89
CHEMBL442423 IC50 = 138.0 nM 6.86
CHEMBL241047 IC50 = 800.0 nM 6.10
CHEMBL193316 IC50 = 1030.0 nM 5.99
CHEMBL240651 IC50 = 1300.0 nM 5.89
CHEMBL240849 IC50 = 2200.0 nM 5.66
CHEMBL240463 IC50 = 2360.0 nM 5.63
CHEMBL240851 IC50 = 11000.0 nM 4.96
CHEMBL392062 IC50 = 12000.0 nM 4.92
CHEMBL240850 IC50 = 49000.0 nM 4.31
CHEMBL241049 IC50 > 100000.0 nM -
CHEMBL391851 IC50 > 100000.0 nM -
CHEMBL393723 IC50 > 100000.0 nM -