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Assay Detail

CHEMBL869795

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

Binding
Inhibition of MMP2
20
Total Activities
20
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

Target

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.
Park K, Aplasca A, Du MT, Sun L, Zhu Y, Zhang Y, Levin JI.
Bioorg Med Chem Lett (2006) 16 : 3927 -3931
PubMed 16723229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.10 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210133 1 8.51
CHEMBL211726 1 7.82
CHEMBL212411 1 7.80
CHEMBL211770 1 7.72
CHEMBL377272 1 7.62
CHEMBL379763 1 7.36
CHEMBL377317 1 7.34
CHEMBL211487 1 7.31
CHEMBL211274 1 7.27
CHEMBL212481 1 7.21
CHEMBL387079 1 7.11
CHEMBL377862 1 6.96
CHEMBL208841 1 6.95
CHEMBL209490 1 6.60
CHEMBL425783 1 6.52
CHEMBL380049 1 6.47
CHEMBL379287 1 6.46
CHEMBL209970 1 6.45
CHEMBL210084 1 6.29
CHEMBL212205 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210133 IC50 = 3.1 nM 8.51
CHEMBL211726 IC50 = 15.0 nM 7.82
CHEMBL212411 IC50 = 16.0 nM 7.80
CHEMBL211770 IC50 = 19.0 nM 7.72
CHEMBL377272 IC50 = 24.0 nM 7.62
CHEMBL379763 IC50 = 44.0 nM 7.36
CHEMBL377317 IC50 = 46.0 nM 7.34
CHEMBL211487 IC50 = 49.0 nM 7.31
CHEMBL211274 IC50 = 54.0 nM 7.27
CHEMBL212481 IC50 = 62.0 nM 7.21
CHEMBL387079 IC50 = 77.0 nM 7.11
CHEMBL377862 IC50 = 111.0 nM 6.96
CHEMBL208841 IC50 = 113.0 nM 6.95
CHEMBL209490 IC50 = 249.0 nM 6.60
CHEMBL425783 IC50 = 302.0 nM 6.52
CHEMBL380049 IC50 = 341.0 nM 6.47
CHEMBL379287 IC50 = 345.0 nM 6.46
CHEMBL209970 IC50 = 355.0 nM 6.45
CHEMBL210084 IC50 = 518.0 nM 6.29
CHEMBL212205 IC50 = 553.0 nM 6.26