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Assay Detail

CHEMBL714222

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

Binding
Inhibitory activity against matrix metalloprotease-2 (MMP-2)
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Xue CB, He X, Roderick J, Corbett RL, Duan JJ, Liu RQ, Covington MB, Qian M, Ribadeneira MD, Vaddi K, Christ DD, Newton RC, Trzaskos JM, Magolda RL, Wexler RR, Decicco CP.
Bioorg Med Chem Lett (2003) 13 : 4299 -4304
PubMed 14643313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.08 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137323 1 6.32
CHEMBL137365 1 6.19
CHEMBL423906 1 6.18
CHEMBL137383 1 6.11
CHEMBL137065 1 6.00
CHEMBL137732 1 5.95
CHEMBL422821 1 5.81
CHEMBL336832 1 -
CHEMBL137297 1 -
CHEMBL341380 1 -
CHEMBL137703 1 -
CHEMBL134908 1 -
CHEMBL137315 1 -
CHEMBL133028 1 -
CHEMBL134782 1 -
CHEMBL133259 1 -
CHEMBL134640 1 -
CHEMBL135766 1 -
CHEMBL342870 1 -
CHEMBL341817 1 -
CHEMBL342687 1 -
CHEMBL135499 1 -
CHEMBL337849 1 -
CHEMBL435399 1 -
CHEMBL137646 1 -
CHEMBL137013 1 -
CHEMBL132928 1 -
CHEMBL343548 1 -
CHEMBL135696 1 -
CHEMBL339380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137323 Ki = 476.0 nM 6.32
CHEMBL137365 Ki = 642.0 nM 6.19
CHEMBL423906 Ki = 656.0 nM 6.18
CHEMBL137383 Ki = 771.0 nM 6.11
CHEMBL137065 Ki = 1002.0 nM 6.00
CHEMBL137732 Ki = 1111.0 nM 5.95
CHEMBL422821 Ki = 1537.0 nM 5.81
CHEMBL341380 Ki > 3333.0 nM -
CHEMBL136353 Ki > 3333.0 nM -
CHEMBL137703 Ki > 3333.0 nM -
CHEMBL134908 Ki > 3333.0 nM -
CHEMBL137315 Ki > 3333.0 nM -
CHEMBL133028 Ki > 3333.0 nM -
CHEMBL134782 Ki > 3333.0 nM -
CHEMBL133259 Ki > 3333.0 nM -
CHEMBL134640 Ki > 3333.0 nM -
CHEMBL135766 Ki > 3333.0 nM -
CHEMBL137297 Ki > 3333.0 nM -
CHEMBL138594 Ki > 3333.0 nM -
CHEMBL344843 Ki > 3333.0 nM -
CHEMBL336832 Ki > 3333.0 nM -
CHEMBL342870 Ki > 2454.0 nM -
CHEMBL341817 Ki > 3333.0 nM -
CHEMBL342687 Ki > 3333.0 nM -
CHEMBL135499 Ki > 3333.0 nM -
CHEMBL337849 Ki > 3333.0 nM -
CHEMBL435399 Ki > 3333.0 nM -
CHEMBL137646 Ki > 3333.0 nM -
CHEMBL137013 Ki > 3333.0 nM -
CHEMBL132928 Ki > 3333.0 nM -
CHEMBL343548 Ki > 1011.0 nM -
CHEMBL135696 Ki > 3333.0 nM -
CHEMBL339380 Ki > 3333.0 nM -