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Assay Detail

CHEMBL3595073

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

Binding
Inhibition of human plasma kallikrein using S2302 as substrate measured for 30 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasma kallikrein (CHEMBL2000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.
Priestley ES, Cheney DL, DeLucca I, Wei A, Luettgen JM, Rendina AR, Wong PC, Wexler RR.
J Med Chem (2015) 58 : 6225 -6236
PubMed 26151189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.96 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3594313 1 7.30
CHEMBL3594314 1 5.77
CHEMBL3594311 1 5.44
CHEMBL3594310 1 5.34
CHEMBL3594312 1 -
CHEMBL3594305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3594313 Ki = 50.0 nM 7.30
CHEMBL3594314 Ki = 1700.0 nM 5.77
CHEMBL3594311 Ki = 3600.0 nM 5.44
CHEMBL3594310 Ki = 4600.0 nM 5.34
CHEMBL3594312 Ki > 6000.0 nM -
CHEMBL3594305 Ki > 6000.0 nM -