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Assay Detail

CHEMBL699546

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

Binding
Tested in vitro for inhibition of human plasma Kallikriene
1
Total Activities
1
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

Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pruitt JR, Pinto DJ, Galemmo RA, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR.
J Med Chem (2003) 46 : 5298 -5315
PubMed 14640539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.24 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151939 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151939 Ki = 58.0 nM 7.24