Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3637200

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

Binding
Inhibition of human trypsin by fluorescence based assay using 25 uM Boc-Gln-Ala-Arg-7-amido-4-methyl coumarinhydrobromide as substrate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.
Goswami R, Wohlfahrt G, Törmäkangas O, Moilanen A, Lakshminarasimhan A, Nagaraj J, Arumugam KN, Mukherjee S, Chacko AR, Krishnamurthy NR, Jaleel M, Palakurthy RK, Samiulla DS, Ramachandra M.
Bioorg Med Chem Lett (2015) 25 : 5309 -5314
PubMed 26421993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.77 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3632759 1 6.40
CHEMBL3632760 1 6.30
CHEMBL3632755 1 6.10
CHEMBL3632761 1 6.10
CHEMBL284805 1 5.10
CHEMBL433501 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3632759 Ki = 400.0 nM 6.40
CHEMBL3632760 Ki = 500.0 nM 6.30
CHEMBL3632755 Ki = 800.0 nM 6.10
CHEMBL3632761 Ki = 800.0 nM 6.10
CHEMBL284805 Ki = 8000.0 nM 5.10
CHEMBL433501 Ki = 23000.0 nM 4.64