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Assay Detail

CHEMBL710331

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

Binding
Inhibition of human fibroblast stromelysin, matrix metalloprotease-3
7
Total Activities
7
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

Novel indolactam-based inhibitors of matrix metalloproteinases
Castelhano AL, Billedeau R, Dewdney N, Donnelly S, Horne S, Kurz LJ, Liak T, Martin R, Uppington R, Zhengyu Yuan, Krantz A
Bioorg Med Chem Lett (1995) 5 : 1415 -1420
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.18 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281795 1 8.05
CHEMBL30980 1 7.82
CHEMBL30804 1 6.09
CHEMBL282146 1 5.35
CHEMBL31164 1 5.18
CHEMBL30782 1 4.60
CHEMBL285112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281795 Ki = 9.0 nM 8.05
CHEMBL30980 Ki = 15.0 nM 7.82
CHEMBL30804 Ki = 806.0 nM 6.09
CHEMBL282146 Ki = 4500.0 nM 5.35
CHEMBL31164 Ki = 6575.0 nM 5.18
CHEMBL30782 Ki = 25000.0 nM 4.60
CHEMBL285112 Ki > 800.0 nM -