Factor Xa inhibitors: next-generation antithrombotic agents.

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Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR

Factor Xa inhibitors: next-generation antithrombotic agents.

J Med Chem. 2010 Sep 9;53(17):6243-74. doi: 10.1021/jm100146h.

PubMed ID
20503967 [ View in PubMed
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Abstract

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DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
3-({4-[(6-CHLORO-1-BENZOTHIEN-2-YL)SULFONYL]-2-OXOPIPERAZIN-1-YL}METHYL)BENZENECARBOXIMIDAMIDECoagulation factor XKi (nM)4N/AN/ADetails
4-{[(E)-2-(5-CHLOROTHIEN-2-YL)VINYL]SULFONYL}-1-(1H-PYRROLO[3,2-C]PYRIDIN-2-YLMETHYL)PIPERAZIN-2-ONECoagulation factor XKi (nM)1.1N/AN/ADetails
5-CHLORO-N-((1R,2S)-2-(4-(2-OXOPYRIDIN-1(2H)-YL)BENZAMIDO) CYCLOPENTYL)THIOPHENE-2-CARBOXAMIDECoagulation factor XKi (nM)0.43N/AN/ADetails
6-CHLORO-N-{(3S)-1-[(1S)-1-METHYL-2-(4-MORPHOLINYL)-2-OXO ETHYL]-2-OXO-3-PYRROLIDINYL}-2-NAPHTHALENESULFONAMIDECoagulation factor XKi (nM)6N/AN/ADetails
ApixabanCoagulation factor XKi (nM)0.08N/AN/ADetails
EribaxabanCoagulation factor XIC 50 (nM)0.32N/AN/ADetails
GW-813893Coagulation factor XKi (nM)4N/AN/ADetails
N-((1R,2R)-2-(5-CHLORO-1H-INDOLE-2-CARBOXAMIDO)CYCLOHEXYL)-5-METHYL-4,5,6,7-TETRAHYDROTHIAZOLO[5,4-C]PYRIDINE-2-CARBOXAMIDECoagulation factor XIC 50 (nM)13N/AN/ADetails
N-((1R,2S)-2-(5-CHLORO-1H-INDOLE-2-CARBOXAMIDO)CYCLOHEXYL)-5-METHYL-4,5,6,7-TETRAHYDROTHIAZOLO[5,4-C]PYRIDINE-2-CARBOXAMIDECoagulation factor XIC 50 (nM)16N/AN/ADetails
OtamixabanCoagulation factor XKi (nM)0.5N/AN/ADetails
RivaroxabanCoagulation factor XKi (nM)0.4N/AN/ADetails
RivaroxabanCoagulation factor XIC 50 (nM)0.7N/AN/ADetails
THIENO[3,2-B]PYRIDINE-2-SULFONIC ACID [1-(1-AMINO-ISOQUINOLIN-7-YLMETHYL)-2-OXO-PYRROLDIN-3-YL]-AMIDECoagulation factor XKi (nM)22N/AN/ADetails
THIENO[3,2-B]PYRIDINE-2-SULFONIC ACID [2-OXO-1-(1H-PYRROLO[2,3-C]PYRIDIN-2-YLMETHYL)-PYRROLIDIN-3-YL]-AMIDECoagulation factor XKi (nM)18N/AN/ADetails