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Assay Detail

CHEMBL765456

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

Binding
Binding affinity was evaluated on serine protease plasma kallikrein.
4
Total Activities
4
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

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP.
J Med Chem (1998) 41 : 3210 -3219
PubMed 9703466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.10 4.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108202 1 4.10
CHEMBL108717 1 -
CHEMBL42495 1 -
CHEMBL441468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108202 Ki = 79000.0 nM 4.10
CHEMBL108717 Ki = 816000.0 nM -
CHEMBL42495 Ki = 586000.0 nM -
CHEMBL441468 Ki = 399000.0 nM -