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Assay Detail

CHEMBL4357416

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

Binding
Inhibition of human activated factor XI using pyro-Glu-Pro-Arg-pNA as substrate by incubated at 25 degreeC spectrophotometry
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor XI (CHEMBL2820)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Corte JR, Pinto DJP, Fang T, Osuna H, Yang W, Wang Y, Lai A, Clark CG, Sun JH, Rampulla R, Mathur A, Kaspady M, Neithnadka PR, Li YC, Rossi KA, Myers JE, Sheriff S, Lou Z, Harper TW, Huang C, Zheng JJ, Bozarth JM, Wu Y, Wong PC, Crain EJ, Seiffert DA, Luettgen JM, Lam PYS, Wexler RR, Ewing WR.
J Med Chem (2020) 63 : 784 -803
PubMed 31833761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.24 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4554665 1 7.33
CHEMBL4522419 2 5.86
CHEMBL4442549 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4554665 Ki = 47.0 nM 7.33
CHEMBL4522419 Ki = 1390.0 nM 5.86
CHEMBL4442549 Ki = 2890.0 nM 5.54
CHEMBL4522419 Ki > 13000.0 nM -