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Assay Detail

CHEMBL3705370

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

Binding
Inhibition Assay: Using a 96 well plate (#3915, Costar), a test compound (25 μL), 400 mM Tris-HCl buffer (pH 8.0, 25 μL) and 0.5 mg/mL fluorescence enzyme substrate (Gly-Asp-Asp-Asp-Asp-Lys-β-Naphtylamide, 25 μL) were mixed, and recombinant human enteropeptidase (R&D Systems, Inc., 25 μL) was added. Using a fluorescence plate reader fmax (Molecular Devices, Inc.), the reaction rate was measured from the time-course changes at excitation wavelength 320 nm and fluorescence wavelength 405 nm.
ChEMBL ↗
81
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Enteropeptidase (CHEMBL1741195) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heteroarylcarboxylic acid ester derivative
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 81 8.97 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5914411 — — 1 9.85
CHEMBL3667883 — — 1 9.62
CHEMBL3672880 — — 1 9.62
CHEMBL3667897 — — 2 9.59
CHEMBL3667902 — — 2 9.57
CHEMBL3667881 — — 1 9.54
CHEMBL3672872 — — 1 9.51
CHEMBL3672887 — — 1 9.41
CHEMBL3667885 — — 1 9.39
CHEMBL3667889 — — 2 9.39
CHEMBL3667882 — — 1 9.34
CHEMBL3667888 — — 1 9.31
CHEMBL3672869 — — 1 9.29
CHEMBL3672877 — — 1 9.28
CHEMBL3672876 — — 1 9.28
CHEMBL3672860 — — 1 9.28
CHEMBL3672886 — — 1 9.24
CHEMBL3672884 — — 1 9.20
CHEMBL3667906 — — 1 9.19
CHEMBL3672857 — — 1 9.17
CHEMBL3672888 — — 1 9.17
CHEMBL3672870 — — 1 9.17
CHEMBL3672889 — — 1 9.16
CHEMBL3667884 — — 1 9.16
CHEMBL3672878 — — 1 9.15
CHEMBL3672871 — — 1 9.15
CHEMBL3672881 — — 1 9.14
CHEMBL3667880 — — 1 9.14
CHEMBL3667905 — — 1 9.14
CHEMBL3667887 — — 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5914411 — Ki = 0.14 nM 9.85
CHEMBL3667883 — Ki = 0.24 nM 9.62
CHEMBL3672880 — Ki = 0.24 nM 9.62
CHEMBL3667897 — Ki = 0.26 nM 9.59
CHEMBL3667902 — Ki = 0.27 nM 9.57
CHEMBL3667881 — Ki = 0.29 nM 9.54
CHEMBL3672872 — Ki = 0.31 nM 9.51
CHEMBL3667897 — Ki = 0.33 nM 9.48
CHEMBL3672887 — Ki = 0.39 nM 9.41
CHEMBL3667885 — Ki = 0.41 nM 9.39
CHEMBL3667889 — Ki = 0.41 nM 9.39
CHEMBL3667902 — Ki = 0.42 nM 9.38
CHEMBL3667882 — Ki = 0.46 nM 9.34
CHEMBL3667888 — Ki = 0.49 nM 9.31
CHEMBL3672869 — Ki = 0.51 nM 9.29
CHEMBL3672877 — Ki = 0.53 nM 9.28
CHEMBL3672876 — Ki = 0.53 nM 9.28
CHEMBL3672860 — Ki = 0.53 nM 9.28
CHEMBL3672886 — Ki = 0.58 nM 9.24
CHEMBL3672884 — Ki = 0.63 nM 9.20
CHEMBL3667906 — Ki = 0.65 nM 9.19
CHEMBL3672870 — Ki = 0.67 nM 9.17
CHEMBL3672857 — Ki = 0.67 nM 9.17
CHEMBL3672888 — Ki = 0.67 nM 9.17
CHEMBL3667884 — Ki = 0.69 nM 9.16
CHEMBL3672889 — Ki = 0.69 nM 9.16
CHEMBL3672871 — Ki = 0.71 nM 9.15
CHEMBL3672878 — Ki = 0.71 nM 9.15
CHEMBL3672881 — Ki = 0.72 nM 9.14
CHEMBL3667880 — Ki = 0.73 nM 9.14
CHEMBL3667905 — Ki = 0.73 nM 9.14
CHEMBL3667887 — Ki = 0.79 nM 9.10
CHEMBL3667893 — Ki = 0.84 nM 9.08
CHEMBL3667899 — Ki = 0.88 nM 9.06
CHEMBL3667886 — Ki = 0.87 nM 9.06
CHEMBL3667889 — Ki = 0.94 nM 9.03
CHEMBL3667908 — Ki = 0.94 nM 9.03
CHEMBL3672850 — Ki = 0.96 nM 9.02
CHEMBL3672851 — Ki = 0.97 nM 9.01
CHEMBL3639717 — Ki = 0.98 nM 9.01
CHEMBL3667892 — Ki = 0.99 nM 9.00
CHEMBL3667895 — Ki = 1.0 nM 9.00
CHEMBL3949541 — Ki = 1.02 nM 8.99
CHEMBL3667909 — Ki = 1.08 nM 8.97
CHEMBL3672882 — Ki = 1.11 nM 8.96
CHEMBL3667894 — Ki = 1.1 nM 8.96
CHEMBL3672874 — Ki = 1.13 nM 8.95
CHEMBL3672891 — Ki = 1.12 nM 8.95
CHEMBL3667907 — Ki = 1.18 nM 8.93
CHEMBL3672893 — Ki = 1.2 nM 8.92