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Assay Detail

CHEMBL3783216

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

Binding
Inhibition of human plasma kallikrein assessed as reduction in release of p-nitroaniline after 10 to 120 mins by Michaelis-Menten equation analysis
4
Total Activities
4
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

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML.
Bioorg Med Chem (2016) 24 : 2257 -2272
PubMed 27073051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.75 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393386 1 7.62
CHEMBL3781788 1 7.38
CHEMBL3780324 1 6.26
CHEMBL3781319 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393386 Ki = 24.0 nM 7.62
CHEMBL3781788 Ki = 42.0 nM 7.38
CHEMBL3780324 Ki = 550.0 nM 6.26
CHEMBL3781319 Ki = 1850.0 nM 5.73