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Assay Detail

CHEMBL930623

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

Binding
Inhibition of pig TACE
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Ott GR, Asakawa N, Lu Z, Liu RQ, Covington MB, Vaddi K, Qian M, Newton RC, Christ DD, Traskos JM, Decicco CP, Duan JJ.
Bioorg Med Chem Lett (2008) 18 : 694 -699
PubMed 18061445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.84 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271235 1 9.85
CHEMBL403401 1 9.40
CHEMBL270800 1 9.03
CHEMBL256805 1 9.00
CHEMBL401263 1 9.00
CHEMBL271234 1 9.00
CHEMBL256621 1 9.00
CHEMBL402746 1 9.00
CHEMBL441901 1 8.96
CHEMBL401979 1 8.89
CHEMBL404162 1 8.82
CHEMBL256598 1 8.82
CHEMBL429589 1 8.80
CHEMBL256245 1 8.80
CHEMBL256681 1 8.80
CHEMBL272341 1 8.74
CHEMBL439066 1 8.70
CHEMBL270819 1 8.68
CHEMBL438528 1 8.64
CHEMBL270606 1 8.57
CHEMBL257532 1 8.34
CHEMBL235997 1 8.20
CHEMBL401824 1 8.20
CHEMBL257531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271235 IC50 = 0.14 nM 9.85
CHEMBL403401 IC50 = 0.4 nM 9.40
CHEMBL270800 IC50 = 0.94 nM 9.03
CHEMBL256805 IC50 = 1.0 nM 9.00
CHEMBL401263 IC50 = 1.0 nM 9.00
CHEMBL271234 IC50 = 1.0 nM 9.00
CHEMBL256621 IC50 = 1.0 nM 9.00
CHEMBL402746 IC50 = 1.0 nM 9.00
CHEMBL441901 IC50 = 1.1 nM 8.96
CHEMBL401979 IC50 = 1.3 nM 8.89
CHEMBL404162 IC50 = 1.5 nM 8.82
CHEMBL256598 IC50 = 1.5 nM 8.82
CHEMBL429589 IC50 = 1.6 nM 8.80
CHEMBL256245 IC50 = 1.6 nM 8.80
CHEMBL256681 IC50 = 1.6 nM 8.80
CHEMBL272341 IC50 = 1.8 nM 8.74
CHEMBL439066 IC50 = 2.0 nM 8.70
CHEMBL270819 IC50 = 2.1 nM 8.68
CHEMBL438528 IC50 = 2.3 nM 8.64
CHEMBL270606 IC50 = 2.7 nM 8.57
CHEMBL257532 IC50 = 4.6 nM 8.34
CHEMBL235997 IC50 = 6.3 nM 8.20
CHEMBL401824 IC50 = 6.3 nM 8.20
CHEMBL257531 IC50 < 1.0 nM -