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Assay Detail

CHEMBL711311

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

Binding
Inhibition of neutrophil collagenase (Matrix metalloprotease-8)
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

Neutrophil collagenase (CHEMBL4588)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Almstead NG, Bradley RS, Pikul S, De B, Natchus MG, Taiwo YO, Gu F, Williams LE, Hynd BA, Janusz MJ, Dunaway CM, Mieling GE.
J Med Chem (1999) 42 : 4547 -4562
PubMed 10579818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.42 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441662 1 9.22
CHEMBL141080 1 9.15
CHEMBL140970 1 8.85
CHEMBL140152 1 8.72
CHEMBL342210 1 8.62
CHEMBL514138 CGS-27023A 1 8.36
CHEMBL1234370 1 6.05
CHEMBL75094 PRINOMASTAT 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441662 IC50 = 0.6 nM 9.22
CHEMBL141080 IC50 = 0.7 nM 9.15
CHEMBL140970 IC50 = 1.4 nM 8.85
CHEMBL140152 IC50 = 1.9 nM 8.72
CHEMBL342210 IC50 = 2.4 nM 8.62
CHEMBL514138 CGS-27023A IC50 = 4.4 nM 8.36
CHEMBL1234370 IC50 = 881.0 nM 6.05
CHEMBL75094 PRINOMASTAT IC50 < 0.4 nM -