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Assay Detail

CHEMBL870697

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

Binding
Binding affinity to recombinant MMP3
8
Total Activities
8
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

Stromelysin-1 (CHEMBL283)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.
Janser P, Neumann U, Miltz W, Feifel R, Buhl T.
Bioorg Med Chem Lett (2006) 16 : 2632 -2636
PubMed 16516469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.68 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72511 1 9.05
CHEMBL382705 1 8.30
CHEMBL207756 1 7.96
CHEMBL208181 1 7.92
CHEMBL115653 CIPEMASTAT 2.0 1 7.25
CHEMBL438964 1 6.73
CHEMBL206875 1 6.52
CHEMBL439330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72511 Ki = 0.9 nM 9.05
CHEMBL382705 Ki = 5.0 nM 8.30
CHEMBL207756 Ki = 11.0 nM 7.96
CHEMBL208181 Ki = 12.0 nM 7.92
CHEMBL115653 CIPEMASTAT Ki = 56.0 nM 7.25
CHEMBL438964 Ki = 187.0 nM 6.73
CHEMBL206875 Ki = 300.0 nM 6.52
CHEMBL439330 Ki - -