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Assay Detail

CHEMBL817753

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

Binding
Inhibitory activity against bovine trypsin
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Serine protease 1 (CHEMBL3769)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Sutton JC, Bolton SA, Davis ME, Hartl KS, Jacobson B, Mathur A, Ogletree ML, Slusarchyk WA, Zahler R, Seiler SM, Bisacchi GS.
Bioorg Med Chem Lett (2004) 14 : 2233 -2239
PubMed 15081015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.21 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71037 1 7.14
CHEMBL70813 1 6.92
CHEMBL73215 1 6.92
CHEMBL431557 1 6.85
CHEMBL70766 1 6.82
CHEMBL72532 1 6.62
CHEMBL70703 1 6.51
CHEMBL70350 1 6.51
CHEMBL304359 1 6.50
CHEMBL72708 1 6.50
CHEMBL69394 1 6.36
CHEMBL70763 1 6.22
CHEMBL71061 1 6.13
CHEMBL305738 1 6.09
CHEMBL304985 1 6.09
CHEMBL302792 1 6.02
CHEMBL305457 1 6.01
CHEMBL429029 1 5.92
CHEMBL72626 1 5.92
CHEMBL69558 1 5.92
CHEMBL70410 1 5.89
CHEMBL419449 1 5.89
CHEMBL70917 1 5.87
CHEMBL72520 1 5.80
CHEMBL70404 1 5.75
CHEMBL70523 1 5.72
CHEMBL70155 1 5.72
CHEMBL303437 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71037 IC50 = 72.0 nM 7.14
CHEMBL70813 IC50 = 120.0 nM 6.92
CHEMBL73215 IC50 = 120.0 nM 6.92
CHEMBL431557 IC50 = 140.0 nM 6.85
CHEMBL70766 IC50 = 150.0 nM 6.82
CHEMBL72532 IC50 = 240.0 nM 6.62
CHEMBL70703 IC50 = 310.0 nM 6.51
CHEMBL70350 IC50 = 310.0 nM 6.51
CHEMBL304359 IC50 = 320.0 nM 6.50
CHEMBL72708 IC50 = 320.0 nM 6.50
CHEMBL69394 IC50 = 440.0 nM 6.36
CHEMBL70763 IC50 = 600.0 nM 6.22
CHEMBL71061 IC50 = 740.0 nM 6.13
CHEMBL305738 IC50 = 810.0 nM 6.09
CHEMBL304985 IC50 = 810.0 nM 6.09
CHEMBL302792 IC50 = 950.0 nM 6.02
CHEMBL305457 IC50 = 970.0 nM 6.01
CHEMBL429029 IC50 = 1200.0 nM 5.92
CHEMBL72626 IC50 = 1200.0 nM 5.92
CHEMBL69558 IC50 = 1200.0 nM 5.92
CHEMBL70410 IC50 = 1300.0 nM 5.89
CHEMBL419449 IC50 = 1300.0 nM 5.89
CHEMBL70917 IC50 = 1350.0 nM 5.87
CHEMBL72520 IC50 = 1580.0 nM 5.80
CHEMBL70404 IC50 = 1800.0 nM 5.75
CHEMBL70523 IC50 = 1900.0 nM 5.72
CHEMBL70155 IC50 = 1900.0 nM 5.72
CHEMBL303437 IC50 = 5760.0 nM 5.24