Assay ID | Title | Year | Journal | Article |
AID633347 | Intrinsic clearance in CD1 mouse liver microsomes assessed as compound remaining at 0.2 uM after 30 mins | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633335 | Anticoagulant activity in mouse plasma assessed as concentration required to double the clotting time by coagulometric analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID1213135 | Drug level in human plasma treated with [14C]darexaban at 60 mg, po | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
| Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. |
AID633334 | Inhibition of human factor 10A using chromogenic substrate S2222 by fluorometric analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633343 | Inhibition of human trypsin using chromogenic substrate S2222 by dixon plot analysis plot | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633342 | Inhibition of human factor 10A using chromogenic substrate S2222 by dixon plot analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633341 | Anticoagulant activity in human plasma assessed as concentration required to double the clotting time by coagulometric analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633348 | Tmax in F344/DuCrlCrlj rat at 100 mg/kg, po assessed as 3-[(4-methoxybenzoyl)amino]-2-{[4-(4-methyl-1,4-diazepan- 1-yl)benzoyl]amino}phenyl beta-D-glucopyranosiduronic acid level after 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID1213138 | Drug level in human intestinal microsomes treated with darexaban at 30 uM after 10 mins by LC-MS/MS analysis in presence of UDPGA | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
| Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. |
AID1213137 | Drug level in human liver microsomes treated with darexaban at 30 uM after 10 mins by LC-MS/MS analysis in presence of UDPGA | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
| Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. |
AID633376 | Cmax in F344/DuCrlCrlj rat at 100 mg/kg, po assessed as 3-[(4-methoxybenzoyl)amino]-2-{[4-(4-methyl-1,4-diazepan- 1-yl)benzoyl]amino}phenyl beta-D-glucopyranosiduronic acid level after 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID1213136 | Tmax in human treated with darexaban at 3 to 720 mg, po | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
| Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. |
AID633377 | AUC (0 to 24 hrs) in F344/DuCrlCrlj rat at 100 mg/kg, po assessed as 3-[(4-methoxybenzoyl)amino]-2-{[4-(4-methyl-1,4-diazepan- 1-yl)benzoyl]amino}phenyl beta-D-glucopyranosiduronic acid level after 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633344 | Inhibition of human thrombin using chromogenic substrate S2238 by dixon plot analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633346 | Effective permeability of the compound after 2 hrs by PAMPA at pH 6.5 | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
AID633345 | Inhibition of human plasma kallikrein using chromogenic substrate S2302 by dixon plot analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |