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Assay Detail

CHEMBL913626

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Binding
Binding affinity to human factor Xa
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Pinto DJ, Galemmo RA, Quan ML, Orwat MJ, Clark C, Li R, Wells B, Woerner F, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, He K, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2006) 16 : 5584 -5589
PubMed 16963264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.96 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378093 1 10.52
CHEMBL373528 1 10.40
CHEMBL374306 1 9.92
CHEMBL221377 1 9.74
CHEMBL221913 1 9.74
CHEMBL222079 1 9.74
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL218723 1 9.70
CHEMBL218525 1 9.46
CHEMBL374305 1 9.14
CHEMBL376710 1 9.13
CHEMBL221296 1 9.12
CHEMBL374187 1 9.09
CHEMBL374304 1 8.92
CHEMBL221968 1 8.70
CHEMBL218659 1 8.70
CHEMBL376227 1 8.59
CHEMBL385756 1 8.57
CHEMBL221092 1 7.92
CHEMBL384769 1 7.70
CHEMBL221911 1 7.33
CHEMBL376622 1 7.27
CHEMBL221028 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378093 Ki = 0.03 nM 10.52
CHEMBL373528 Ki = 0.04 nM 10.40
CHEMBL374306 Ki = 0.12 nM 9.92
CHEMBL221377 Ki = 0.18 nM 9.74
CHEMBL221913 Ki = 0.18 nM 9.74
CHEMBL222079 Ki = 0.18 nM 9.74
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL218723 Ki = 0.2 nM 9.70
CHEMBL218525 Ki = 0.35 nM 9.46
CHEMBL374305 Ki = 0.72 nM 9.14
CHEMBL376710 Ki = 0.74 nM 9.13
CHEMBL221296 Ki = 0.76 nM 9.12
CHEMBL374187 Ki = 0.82 nM 9.09
CHEMBL374304 Ki = 1.2 nM 8.92
CHEMBL221968 Ki = 2.0 nM 8.70
CHEMBL218659 Ki = 2.0 nM 8.70
CHEMBL376227 Ki = 2.6 nM 8.59
CHEMBL385756 Ki = 2.7 nM 8.57
CHEMBL221092 Ki = 12.0 nM 7.92
CHEMBL384769 Ki = 20.0 nM 7.70
CHEMBL221911 Ki = 47.0 nM 7.33
CHEMBL376622 Ki = 54.0 nM 7.27
CHEMBL221028 Ki = 88.0 nM 7.06