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Assay Detail

CHEMBL822190

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

Binding
Activity against deletion mutant of MT1-MMP lacking the transmembrane domain (deltaMT1)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Matrix metalloproteinase-14 (CHEMBL3869)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.
Yamamoto M, Tsujishita H, Hori N, Ohishi Y, Inoue S, Ikeda S, Okada Y.
J Med Chem (1998) 41 : 1209 -1217
PubMed 9548812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.09 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279785 MARIMASTAT 3.0 1 8.74
CHEMBL16520 RO-319790 1 8.72
CHEMBL20154 1 8.72
CHEMBL279078 1 8.68
CHEMBL281371 1 8.64
CHEMBL20043 1 8.60
CHEMBL279786 BATIMASTAT 2.0 1 8.52
CHEMBL432842 1 8.07
CHEMBL19932 1 7.89
CHEMBL19611 ILOMASTAT 2.0 1 7.87
CHEMBL433426 1 7.75
CHEMBL279964 1 7.71
CHEMBL19843 1 7.25
CHEMBL433816 1 7.14
CHEMBL19623 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279785 MARIMASTAT IC50 = 1.82 nM 8.74
CHEMBL16520 RO-319790 IC50 = 1.9 nM 8.72
CHEMBL20154 IC50 = 1.9 nM 8.72
CHEMBL279078 IC50 = 2.08 nM 8.68
CHEMBL281371 IC50 = 2.3 nM 8.64
CHEMBL20043 IC50 = 2.5 nM 8.60
CHEMBL279786 BATIMASTAT IC50 = 3.0 nM 8.52
CHEMBL432842 IC50 = 8.5 nM 8.07
CHEMBL19932 IC50 = 13.0 nM 7.89
CHEMBL19611 ILOMASTAT IC50 = 13.4 nM 7.87
CHEMBL433426 IC50 = 17.6 nM 7.75
CHEMBL279964 IC50 = 19.3 nM 7.71
CHEMBL19843 IC50 = 56.0 nM 7.25
CHEMBL433816 IC50 = 72.0 nM 7.14
CHEMBL19623 IC50 = 105.0 nM 6.98