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Assay Detail

CHEMBL3371671

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

Binding
Inhibition of human recombinant matriptase-2 using Boc-Gln-Ala-Arg-AMC as substrate by microplate reader analysis
15
Total Activities
15
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

Transmembrane protease serine 6 (CHEMBL1795139)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptase and matriptase-2.
Duchêne D, Colombo E, Désilets A, Boudreault PL, Leduc R, Marsault E, Najmanovich R.
J Med Chem (2014) 57 : 10198 -10204
PubMed 25387268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.15 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354675 1 9.13
CHEMBL3354683 1 8.99
CHEMBL3354676 1 8.85
CHEMBL3354685 1 8.70
CHEMBL3354686 1 8.61
CHEMBL3354684 1 8.59
CHEMBL3354677 1 8.20
CHEMBL3354674 1 8.11
CHEMBL3354679 1 7.87
CHEMBL3354678 1 7.81
CHEMBL3354687 1 7.68
CHEMBL3354682 1 7.61
CHEMBL3352840 1 7.46
CHEMBL3354680 1 7.33
CHEMBL3354681 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354675 Ki = 0.74 nM 9.13
CHEMBL3354683 Ki = 1.03 nM 8.99
CHEMBL3354676 Ki = 1.4 nM 8.85
CHEMBL3354685 Ki = 1.98 nM 8.70
CHEMBL3354686 Ki = 2.48 nM 8.61
CHEMBL3354684 Ki = 2.56 nM 8.59
CHEMBL3354677 Ki = 6.3 nM 8.20
CHEMBL3354674 Ki = 7.8 nM 8.11
CHEMBL3354679 Ki = 13.47 nM 7.87
CHEMBL3354678 Ki = 15.4 nM 7.81
CHEMBL3354687 Ki = 20.79 nM 7.68
CHEMBL3354682 Ki = 24.84 nM 7.61
CHEMBL3352840 Ki = 34.8 nM 7.46
CHEMBL3354680 Ki = 46.78 nM 7.33
CHEMBL3354681 Ki = 47.77 nM 7.32