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Assay Detail

CHEMBL2020839

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

Binding
Inhibition of plasma kallikrein by dixon plot method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Plasma kallikrein (CHEMBL2000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new strategy for the development of highly potent and selective plasmin inhibitors.
Saupe SM, Steinmetzer T.
J Med Chem (2012) 55 : 1171 -1180
PubMed 22276953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.65 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2016865 1 10.12
CHEMBL2016873 1 8.62
CHEMBL2016871 1 8.03
CHEMBL2016874 1 8.00
CHEMBL2016870 1 7.76
CHEMBL2016872 1 7.72
CHEMBL2016869 1 7.60
CHEMBL2016866 1 7.59
CHEMBL2016875 1 7.17
CHEMBL2016868 1 6.87
CHEMBL2016867 1 6.31
CHEMBL2016864 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2016865 Ki = 0.075 nM 10.12
CHEMBL2016873 Ki = 2.4 nM 8.62
CHEMBL2016871 Ki = 9.4 nM 8.03
CHEMBL2016874 Ki = 10.1 nM 8.00
CHEMBL2016870 Ki = 17.4 nM 7.76
CHEMBL2016872 Ki = 19.0 nM 7.72
CHEMBL2016869 Ki = 25.3 nM 7.60
CHEMBL2016866 Ki = 25.4 nM 7.59
CHEMBL2016875 Ki = 67.0 nM 7.17
CHEMBL2016868 Ki = 136.0 nM 6.87
CHEMBL2016867 Ki = 493.0 nM 6.31
CHEMBL2016864 Ki = 868.0 nM 6.06