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Assay Detail

CHEMBL710334

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

Binding
Inhibition of human fibroblast stromelysin, matrix metalloprotease-3
10
Total Activities
10
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

Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1 heteroatom based modifications
Tomczuk BE, Gowravaram MR, Johnson JS, Delecki D, Cook ER, Ghose AK, Mathiowetz AM, Spurlino JC, Rubin B, Smith DL, Pulvino T, Wahl RC
Bioorg Med Chem Lett (1995) 5 : 343 -348
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.15 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86797 1 8.22
CHEMBL59023 1 7.85
CHEMBL87229 1 7.82
CHEMBL410259 1 7.55
CHEMBL313483 1 7.37
CHEMBL430838 1 7.04
CHEMBL85766 1 6.44
CHEMBL87046 1 6.37
CHEMBL86468 1 5.66
CHEMBL85933 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86797 Ki = 6.0 nM 8.22
CHEMBL59023 Ki = 14.0 nM 7.85
CHEMBL87229 Ki = 15.0 nM 7.82
CHEMBL410259 Ki = 28.0 nM 7.55
CHEMBL313483 Ki = 43.0 nM 7.37
CHEMBL430838 Ki = 92.0 nM 7.04
CHEMBL85766 Ki = 360.0 nM 6.44
CHEMBL87046 Ki = 430.0 nM 6.37
CHEMBL86468 Ki = 2200.0 nM 5.66
CHEMBL85933 Ki > 10000.0 nM -