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Assay Detail

CHEMBL661586

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Binding
Inhibition of Coagulation factor Xa
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW.
Bioorg Med Chem Lett (2002) 12 : 1671 -1674
PubMed 12039587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.67 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46618 OTAMIXABAN 3.0 1 9.40
CHEMBL296046 1 9.30
CHEMBL46708 1 9.24
CHEMBL295454 1 9.10
CHEMBL295010 1 9.05
CHEMBL44586 1 8.92
CHEMBL46969 1 8.70
CHEMBL47207 1 8.57
CHEMBL44113 1 8.52
CHEMBL45000 1 8.28
CHEMBL45307 1 8.22
CHEMBL415907 1 8.10
CHEMBL45298 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46618 OTAMIXABAN Ki = 0.4 nM 9.40
CHEMBL296046 Ki = 0.5 nM 9.30
CHEMBL46708 Ki = 0.58 nM 9.24
CHEMBL295454 Ki = 0.8 nM 9.10
CHEMBL295010 Ki = 0.89 nM 9.05
CHEMBL44586 Ki = 1.2 nM 8.92
CHEMBL46969 Ki = 2.0 nM 8.70
CHEMBL47207 Ki = 2.7 nM 8.57
CHEMBL44113 Ki = 3.0 nM 8.52
CHEMBL45000 Ki = 5.3 nM 8.28
CHEMBL45307 Ki = 6.0 nM 8.22
CHEMBL415907 Ki = 8.0 nM 8.10
CHEMBL45298 Ki = 46.0 nM 7.34