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Assay Detail

CHEMBL3756038

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

Binding
Inhibition of Bacillus thermoproteolyticus thermolysin pretreated with compound for 1 hr followed by the addition of 3.33 uM bradykinin like substrate by spectrofluorometry assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus thermoproteolyticus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thermolysin (CHEMBL3392)
Type SINGLE PROTEIN
Organism Bacillus thermoproteolyticus

Publication

Synthesis, experimental evaluation and molecular modelling of hydroxamate derivatives as zinc metalloproteinase inhibitors.
Sjøli S, Nuti E, Camodeca C, Bilto I, Rossello A, Winberg JO, Sylte I, Adekoya OA.
Eur J Med Chem (2016) 108 : 141 -153
PubMed 26638045 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.69 5.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228230 1 5.02
CHEMBL3754100 1 4.54
CHEMBL3753984 1 4.52
CHEMBL3752513 1 -
CHEMBL3752374 1 -
CHEMBL3751971 1 -
CHEMBL573714 1 -
CHEMBL3754094 1 -
CHEMBL1090284 1 -
CHEMBL179288 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228230 IC50 = 9500.0 nM 5.02
CHEMBL3754100 IC50 = 29000.0 nM 4.54
CHEMBL3753984 IC50 = 30000.0 nM 4.52
CHEMBL3752513 IC50 = 438000.0 nM -
CHEMBL3752374 IC50 - -
CHEMBL3751971 IC50 = 132000.0 nM -
CHEMBL573714 IC50 = 146000.0 nM -
CHEMBL3754094 IC50 = 608000.0 nM -
CHEMBL1090284 IC50 - -
CHEMBL179288 IC50 = 800000.0 nM -