Assay ID | Title | Year | Journal | Article |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1219531 | AUC (0 to infinity) in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219411 | AUC (0 to infinity) in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219529 | Inhibition of GSK3beta (unknown origin) | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219530 | Inhibition of GSK3alpha (unknown origin) | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219454 | Cmax in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219457 | Cmax in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219534 | Clearance in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219468 | Tmax in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID241315 | Inhibition of human Mitogen-activated protein kinase p38 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219478 | Plasma protein binding in rat | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219385 | Drug recovery in bile duct-intact Sprague-Dawley rat assessed as radioactivity in feces during 0 to 24 hrs at 5 mg/kg, iv for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1537911 | Inhibition of human GSK-3alpha S449A mutant (2 to end residues) using phospho GS2 peptide as substrate after 40 mins in presence of [gamma-33ATP] by scintillation counting method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219503 | Ratio of drug level in blood to plasma in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219459 | Cmax in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219453 | Cmax in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219525 | Drug recovery in beagle dog feces at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1537913 | Inhibition of human GSK-3beta H350L mutant (2 to end residues) at 10 uM using phospho GS2 peptide as substrate after 40 mins by [gamma-33ATP] radiometric assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219417 | Clearance in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1537912 | Inhibition of human GSK-3beta H350L mutant (2 to end residues) at 10 uM using phospho GS2 peptide as substrate after 40 mins by [gamma-33ATP] radiometric assay relative to control | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219524 | Elimination half life in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219521 | Tmax in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219425 | Clearance in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240968 | Inhibition of human TGF-beta type II receptor | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219544 | Drug recovery in Sprague-Dawley rat feces at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219412 | AUC (0 to infinity) in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219410 | AUC (0 to infinity) in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240520 | Inhibition of human MLK7 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219432 | Volume of distribution at steady state in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219509 | Drug recovery in beagle dog plasma assessed as radiochemical peak area at 5 mg/kg, iv administered for 30 mins after 0.5 hrs by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219381 | Drug recovery in cancer patient at 80 to 120 mg for 60 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219547 | Drug recovery in Sprague-Dawley rat cage at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219492 | Drug metabolism in Mdr1a knockout Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1537910 | Inhibition of human GSK-3alpha S449A mutant (2 to end residues) at 10 uM using phospho GS2 peptide as substrate after 40 mins in presence of [gamma-33ATP] by scintillation counting method relative to control | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219535 | Volume of distribution at steady state in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219404 | AUC (0 to infinity) in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219429 | Volume of distribution at steady state in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219507 | Drug recovery in bile duct-cannulated Sprague-Dawley rat assessed as radioactivity in bile during 0 to 12 hrs at 5 mg/kg, iv for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID242896 | Threshold minimal effective dose in rats | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219414 | AUC (0 to infinity) in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219397 | Drug recovery in bile duct-cannulated Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins during 0 to 12 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219471 | Tmax in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID237961 | Compound was tested for volume distribution | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219546 | Drug recovery in Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219408 | AUC (0 to infinity) in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219428 | Volume of distribution at steady state in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219380 | Ratio of AUC (0 to infinity) to AUC (0 to 6 hrs) in cancer patient at 80 to 120 mg for 60 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219422 | Clearance in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219550 | Drug recovery in bile duct-cannulated Sprague-Dawley rat cage/carcass at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219511 | Total drug recovery in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID243296 | In vivo glucose reduction in rats at 10 mg/kg dose | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219426 | Clearance in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID237621 | Compound was tested for in vivo clearance | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219440 | Half life in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219520 | Cmax in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219493 | Drug metabolism in Bcrp knockout Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID243424 | In vivo insulin (10 units) response in rats at 10 mg/kg dose | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219482 | Ratio of drug level in blood to plasma in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219445 | Half life in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219423 | Clearance in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219481 | Ratio of drug level in blood to plasma in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219466 | Tmax in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219496 | Drug metabolism in Bcrp knockout Sprague-Dawley rat bile at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240881 | Inhibition of human Protein kinase C beta 2 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219396 | Drug recovery in bile duct-cannulated Sprague-Dawley rat feces at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219484 | Drug recovery in bile duct-cannulated Sprague-Dawley rat assessed as radioactivity in bile during 0 to 24 hrs at 5 mg/kg, iv administered for 30 mins relative to dosed radioactivity | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219518 | Elimination half life in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219532 | Cmax in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240966 | Inhibition of human Cyclin-dependent kinase 2 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219461 | Cmax in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219401 | Tmax in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219537 | AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219402 | Tmax in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219485 | Drug recovery in bile duct-cannulated Sprague-Dawley rat assessed as radioactivity in feces during 0 to 24 hrs at 5 mg/kg, iv administered for 30 mins relative to dosed radioactivity | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219383 | Ratio of glomerular filtration rate to renal clearance in cancer patient at 80 to 120 mg for 60 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219382 | Clearance in cancer patient kidney at 80 to 120 mg for 60 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219436 | Volume of distribution at steady state in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219418 | Clearance in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219476 | Total drug recovery in beagle dog at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240855 | Inhibition of human Protein kinase A beta | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219421 | Clearance in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219456 | Cmax in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219526 | Drug recovery in beagle dog feces at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219515 | Tmax in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219483 | Drug recovery in bile duct-cannulated Sprague-Dawley rat assessed as radioactivity in bile during 0 to 12 hrs at 5 mg/kg, iv administered for 30 mins relative to dosed radioactivity | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240967 | Inhibition of human Cyclin-dependent kinase 4 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219431 | Volume of distribution at steady state in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219517 | Volume of distribution at steady state in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219536 | Elimination half life in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219541 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219437 | Volume of distribution at steady state in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219543 | Drug recovery in Sprague-Dawley rat feces at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219467 | Tmax in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219495 | Drug metabolism in Mdr1a knockout Sprague-Dawley rat bile at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219460 | Cmax in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219399 | Drug recovery in bile duct-cannulated Sprague-Dawley rat bile at 5 mg/kg, iv administered for 30 mins during 0 to 12 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219378 | Half life in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219552 | Total drug recovery in bile duct-cannulated Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219438 | Volume of distribution at steady state in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1537907 | Inhibition of human GSK-3beta using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured in presence of [gamma-33P]ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219403 | Tmax in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219472 | Tmax in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219538 | Cmax in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219510 | Drug recovery in beagle dog plasma assessed as radiochemical peak area at 5 mg/kg, iv administered for 30 mins after 2 hrs by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID241157 | Inhibition of human Glycogen synthase kinase-3 beta | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219409 | AUC (0 to infinity) in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219462 | Cmax in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID241585 | Inhibition of human Vascular endothelial growth factor receptor 2 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219447 | Half life in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219433 | Volume of distribution at steady state in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219443 | Half life in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219458 | Cmax in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219498 | Plasma protein binding in beagle dog | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240545 | Inhibition of human PDK-1 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219465 | Tmax in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219489 | Drug metabolism in Mdr1a knockout Sprague-Dawley rat plasma at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219549 | Drug recovery in Sprague-Dawley rat carcass at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219475 | Drug recovery in beagle dog cage at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219424 | Clearance in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219522 | Clearance in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219415 | AUC (0 to infinity) in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219551 | Total drug recovery in bile duct-cannulated Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins during 0 to 12 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219464 | Cmax in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219455 | Cmax in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219512 | Total drug recovery in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219470 | Tmax in cancer patient at 120 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219499 | Total drug recovery in beagle dog at 5 mg/kg, iv administered for 30 mins during 48 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID237101 | Half life in in vivo, hours | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219469 | Tmax in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219419 | Clearance in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219491 | Drug metabolism in Mrp2 knockout Sprague-Dawley rat plasma at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219442 | Half life in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219494 | Drug metabolism in Mrp2 knockout Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219413 | AUC (0 to infinity) in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219473 | Tmax in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID242597 | Inhibition of Glycogen synthase kinase-3 beta dependent Tau protein serine-396 phosphorylation in human SY5Y cells | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219444 | Half life in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219379 | Half life in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219523 | Volume of distribution at steady state in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219434 | Volume of distribution at steady state in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219384 | Plasma protein binding in cancer patient | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219446 | Half life in cancer patient at 10 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219416 | Clearance in cancer patient at 10 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219540 | Clearance in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219490 | Drug metabolism in Bcrp knockout Sprague-Dawley rat plasma at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID241780 | Inhibition of human Calcium/calmodulin-dependent protein kinase type II | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219406 | AUC (0 to infinity) in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID240519 | Inhibition of human Akt1 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219441 | Half life in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219405 | AUC (0 to infinity) in cancer patient at 20 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219501 | Drug uptake in beagle dog rat blood at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219480 | Drug uptake in Sprague-Dawley rat blood at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219505 | Drug recovery in Sprague-Dawley rat feces at 5 mg/kg, iv administered for 30 mins during 48 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219486 | Drug recovery in bile duct-intact beagle dog assessed as radioactivity in feces during 0 to 48 hrs at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219497 | Drug metabolism in Mrp2 knockout Sprague-Dawley rat bile at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219439 | Volume of distribution at steady state in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219519 | AUC (0 to infinity) in beagle dog assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219487 | Drug recovery in bile duct-intact Sprague-Dawley rat assessed as radioactivity in feces during 0 to 24 hrs at 5 mg/kg, iv administered for 30 mins relative to dosed radioactivity | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219479 | Plasma concentration in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219398 | Drug recovery in bile duct-cannulated Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219488 | Drug recovery in bile duct-intact Sprague-Dawley rat assessed as radioactivity in bile during 0 to 24 hrs at 5 mg/kg, iv administered for 30 mins relative to dosed radioactivity | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219427 | Clearance in cancer patient at 120 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219430 | Volume of distribution at steady state in cancer patient at 40 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219502 | Ratio of drug level in blood to plasma in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID236338 | Compound was tested for oral AUC at 0 to 24 hours | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1537906 | Inhibition of human GSK-3alpha using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured in presence of [gamma-33P]ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. |
AID1219463 | Cmax in cancer patient at 80 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID419615 | Inhibition of human GSK3-beta | 2009 | European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
| Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. |
AID1219407 | AUC (0 to infinity) in cancer patient at 60 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219451 | Drug recovery in beagle dog urine at 5 mg/kg, iv administered for 30 mins during 0 to 12 hrs by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219542 | Elimination half life in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219533 | Tmax in Sprague-Dawley rat assessed as total radioactivity at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219527 | Drug recovery in beagle dog urine at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219528 | Drug recovery in beagle dog urine at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219477 | Total drug recovery in beagle dog at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219539 | Tmax in Sprague-Dawley rat at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219514 | Cmax in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219548 | Drug recovery in Sprague-Dawley rat cage at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219474 | Drug recovery in beagle dog cage at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219400 | Drug recovery in bile duct-cannulated Sprague-Dawley rat bile at 5 mg/kg, iv administered for 30 mins during 0 to 168 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219377 | Half life in cancer patient at 60 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219500 | Plasma concentration in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID237845 | Oral bioavailability | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1219448 | Half life in cancer patient at 40 mg for 60 mins treated 1/8 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219516 | Clearance in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219513 | AUC (0 to infinity) in beagle dog at 5 mg/kg, iv administered for 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219435 | Volume of distribution at steady state in cancer patient at 20 mg for 60 mins treated 2/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219420 | Clearance in cancer patient at 80 mg for 60 mins treated 1/1 cycle/day | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219504 | Plasma concentration in beagle dog at Tmax | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID1219545 | Drug recovery in Sprague-Dawley rat urine at 5 mg/kg, iv administered for 30 mins during 0 to 24 hrs time interval by radio analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. |
AID237090 | Half life in oral, hours | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1345633 | Human glycogen synthase kinase 3 beta (GSK subfamily) | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |