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Assay Detail

CHEMBL712567

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

Binding
Inhibition of matrix metalloprotease-9, gelatinase-B
9
Total Activities
9
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

Matrix metalloproteinase-9 (CHEMBL321)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.
Levin JI, DiJoseph JF, Killar LM, Sharr MA, Skotnicki JS, Patel DV, Xiao XY, Shi L, Navre M, Campbell DA.
Bioorg Med Chem Lett (1998) 8 : 1163 -1168
PubMed 9871728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.18 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16519 1 9.85
CHEMBL16554 1 9.85
CHEMBL16630 1 8.10
CHEMBL16933 1 8.10
CHEMBL16520 RO-319790 1 7.92
CHEMBL16650 1 7.92
CHEMBL16595 1 7.70
CHEMBL17082 1 7.62
CHEMBL16505 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16519 IC50 = 0.14 nM 9.85
CHEMBL16554 IC50 = 0.14 nM 9.85
CHEMBL16630 IC50 = 8.0 nM 8.10
CHEMBL16933 IC50 = 8.0 nM 8.10
CHEMBL16520 RO-319790 IC50 = 12.0 nM 7.92
CHEMBL16650 IC50 = 12.0 nM 7.92
CHEMBL16595 IC50 = 20.0 nM 7.70
CHEMBL17082 IC50 = 24.0 nM 7.62
CHEMBL16505 IC50 = 250.0 nM 6.60