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Assay Detail

CHEMBL902120

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Binding
Inhibition of MMP12
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Macrophage metalloelastase (CHEMBL4393)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 28 6.21 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240465 1 7.30
CHEMBL391288 1 6.89
CHEMBL240464 1 6.68
CHEMBL440048 1 6.41
CHEMBL248173 1 6.24
CHEMBL391376 1 5.99
CHEMBL395880 1 5.99
CHEMBL429112 1 5.89
CHEMBL240854 1 5.39
CHEMBL240855 1 5.33
CHEMBL442423 1 -
CHEMBL248172 1 -
CHEMBL392867 1 -
CHEMBL247966 1 -
CHEMBL241051 1 -
CHEMBL393944 1 -
CHEMBL428212 1 -
CHEMBL247967 1 -
CHEMBL395878 1 -
CHEMBL395877 1 -
CHEMBL240648 1 -
CHEMBL438125 1 -
CHEMBL240852 1 -
CHEMBL240654 1 -
CHEMBL427861 1 -
CHEMBL240653 1 -
CHEMBL241048 1 -
CHEMBL240652 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240465 Ki = 50.0 nM 7.30
CHEMBL391288 Ki = 130.0 nM 6.89
CHEMBL240464 Ki = 210.0 nM 6.68
CHEMBL440048 Ki = 390.0 nM 6.41
CHEMBL248173 Ki = 580.0 nM 6.24
CHEMBL391376 Ki = 1030.0 nM 5.99
CHEMBL395880 Ki = 1020.0 nM 5.99
CHEMBL429112 Ki = 1290.0 nM 5.89
CHEMBL240854 Ki = 4100.0 nM 5.39
CHEMBL240855 Ki = 4640.0 nM 5.33
CHEMBL442423 Ki - -
CHEMBL248172 Ki > 4040.0 nM -
CHEMBL392867 Ki > 6020.0 nM -
CHEMBL247966 Ki > 6020.0 nM -
CHEMBL241051 Ki > 6020.0 nM -
CHEMBL393944 Ki > 6020.0 nM -
CHEMBL428212 Ki > 6020.0 nM -
CHEMBL247967 Ki - -
CHEMBL395878 Ki > 6020.0 nM -
CHEMBL395877 Ki > 6020.0 nM -
CHEMBL240648 Ki > 6020.0 nM -
CHEMBL438125 Ki > 6020.0 nM -
CHEMBL240852 Ki > 6020.0 nM -
CHEMBL240654 Ki > 6020.0 nM -
CHEMBL427861 Ki > 6020.0 nM -
CHEMBL240653 Ki > 6020.0 nM -
CHEMBL241048 Ki > 6020.0 nM -
CHEMBL240652 Ki > 6020.0 nM -