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Assay Detail

CHEMBL3371468

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

Binding
Inhibition of purified human factor Xa
17
Total Activities
17
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 X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.
Bioorg Med Chem Lett (2014) 24 : 3341 -3345
PubMed 24951330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.59 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314447 1 10.30
CHEMBL3359592 1 10.30
CHEMBL3314448 1 10.22
CHEMBL3314454 1 10.15
CHEMBL3314445 1 10.15
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL3314442 1 9.96
CHEMBL3314450 1 9.82
CHEMBL3314453 1 9.70
CHEMBL3314443 1 9.62
CHEMBL3314444 1 9.49
CHEMBL3314455 1 9.32
CHEMBL3314440 1 9.18
CHEMBL3314441 1 9.00
CHEMBL3314449 1 8.91
CHEMBL3314451 1 8.82
CHEMBL3314452 1 8.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314447 Ki = 0.05 nM 10.30
CHEMBL3359592 Ki = 0.05 nM 10.30
CHEMBL3314448 Ki = 0.06 nM 10.22
CHEMBL3314454 Ki = 0.07 nM 10.15
CHEMBL3314445 Ki = 0.07 nM 10.15
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL3314442 Ki = 0.11 nM 9.96
CHEMBL3314450 Ki = 0.15 nM 9.82
CHEMBL3314453 Ki = 0.2 nM 9.70
CHEMBL3314443 Ki = 0.24 nM 9.62
CHEMBL3314444 Ki = 0.32 nM 9.49
CHEMBL3314455 Ki = 0.48 nM 9.32
CHEMBL3314440 Ki = 0.66 nM 9.18
CHEMBL3314441 Ki = 1.01 nM 9.00
CHEMBL3314449 Ki = 1.22 nM 8.91
CHEMBL3314451 Ki = 1.5 nM 8.82
CHEMBL3314452 Ki = 9.27 nM 8.03