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Assay Detail

CHEMBL897708

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Binding
Inhibition of human recombinant MMP2
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Huang A, Joseph-McCarthy D, Lovering F, Sun L, Wang W, Xu W, Zhu Y, Cui J, Zhang Y, Levin JI.
Bioorg Med Chem (2007) 15 : 6170 -6181
PubMed 17606376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.66 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207729 1 8.33
CHEMBL236400 1 7.34
CHEMBL238081 1 7.25
CHEMBL237467 1 7.01
CHEMBL236573 1 6.92
CHEMBL399401 1 6.67
CHEMBL209970 1 6.55
CHEMBL399400 1 6.48
CHEMBL235559 1 6.29
CHEMBL400430 1 5.88
CHEMBL237468 1 5.82
CHEMBL236806 1 5.38
CHEMBL394003 1 -
CHEMBL237466 1 -
CHEMBL236574 1 -
CHEMBL236572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207729 IC50 = 4.7 nM 8.33
CHEMBL236400 IC50 = 46.0 nM 7.34
CHEMBL238081 IC50 = 56.0 nM 7.25
CHEMBL237467 IC50 = 97.0 nM 7.01
CHEMBL236573 IC50 = 120.0 nM 6.92
CHEMBL399401 IC50 = 216.0 nM 6.67
CHEMBL209970 IC50 = 280.0 nM 6.55
CHEMBL399400 IC50 = 334.0 nM 6.48
CHEMBL235559 IC50 = 513.0 nM 6.29
CHEMBL400430 IC50 = 1312.0 nM 5.88
CHEMBL237468 IC50 = 1530.0 nM 5.82
CHEMBL236806 IC50 = 4181.0 nM 5.38
CHEMBL394003 IC50 > 1666.0 nM -
CHEMBL237466 IC50 - -
CHEMBL236574 IC50 - -
CHEMBL236572 IC50 - -