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Assay Detail

CHEMBL2446582

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

Binding
Inhibition of human recombinant MMP-2 using MOCAcPLGLA2pr(Dnp)AR-NH2 as substrate by fluorescence spectrophotometric analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.
Gooyit M, Song W, Mahasenan KV, Lichtenwalter K, Suckow MA, Schroeder VA, Wolter WR, Mobashery S, Chang M.
J Med Chem (2013) 56 : 8139 -8150
PubMed 24028490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.55 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2063274 1 8.22
CHEMBL2442885 1 7.30
CHEMBL2442889 1 6.80
CHEMBL2442890 1 6.64
CHEMBL2442881 1 6.62
CHEMBL2442886 1 6.54
CHEMBL2442891 1 6.51
CHEMBL2442893 1 6.41
CHEMBL2442884 1 6.38
CHEMBL2442882 1 6.36
CHEMBL2442892 1 6.32
CHEMBL2442887 1 6.31
CHEMBL2442878 1 6.26
CHEMBL2442883 1 6.25
CHEMBL2442888 1 6.17
CHEMBL2442880 1 6.16
CHEMBL2442879 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2063274 Ki = 6.0 nM 8.22
CHEMBL2442885 Ki = 50.0 nM 7.30
CHEMBL2442889 Ki = 160.0 nM 6.80
CHEMBL2442890 Ki = 230.0 nM 6.64
CHEMBL2442881 Ki = 240.0 nM 6.62
CHEMBL2442886 Ki = 290.0 nM 6.54
CHEMBL2442891 Ki = 310.0 nM 6.51
CHEMBL2442893 Ki = 390.0 nM 6.41
CHEMBL2442884 Ki = 420.0 nM 6.38
CHEMBL2442882 Ki = 440.0 nM 6.36
CHEMBL2442892 Ki = 480.0 nM 6.32
CHEMBL2442887 Ki = 490.0 nM 6.31
CHEMBL2442878 Ki = 550.0 nM 6.26
CHEMBL2442883 Ki = 560.0 nM 6.25
CHEMBL2442888 Ki = 680.0 nM 6.17
CHEMBL2442880 Ki = 690.0 nM 6.16
CHEMBL2442879 Ki = 760.0 nM 6.12