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Assay Detail

CHEMBL3854656

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

Binding
Inhibition of human factor 11a using pyroGlu-Pro-Arg-pNA as substrate assessed as release of pNA after 10 to 120 mins by spectrophotometric method
11
Total Activities
11
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

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES.
J Med Chem (2016) 59 : 7125 -7137
PubMed 27455395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.40 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3978562 1 5.85
CHEMBL3891120 1 5.64
CHEMBL3980787 1 5.54
CHEMBL3951940 1 5.51
CHEMBL3902498 1 5.47
CHEMBL3917434 1 5.21
CHEMBL3926417 1 5.19
CHEMBL3942944 1 5.15
CHEMBL3935309 1 5.06
CHEMBL3930523 1 -
CHEMBL3907376 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3978562 Ki = 1400.0 nM 5.85
CHEMBL3891120 Ki = 2300.0 nM 5.64
CHEMBL3980787 Ki = 2900.0 nM 5.54
CHEMBL3951940 Ki = 3100.0 nM 5.51
CHEMBL3902498 Ki = 3400.0 nM 5.47
CHEMBL3917434 Ki = 6100.0 nM 5.21
CHEMBL3926417 Ki = 6500.0 nM 5.19
CHEMBL3942944 Ki = 7100.0 nM 5.15
CHEMBL3935309 Ki = 8800.0 nM 5.06
CHEMBL3930523 Ki > 10000.0 nM -
CHEMBL3907376 Ki > 10000.0 nM -