| Assay ID | Title | Year | Journal | Article |
|---|
| AID750512 | Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750486 | Inhibition of human VPS34 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280827 | Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1280832 | Antiproliferative activity against human MCF7-neo/Her2 cells after 3 days by luminescence plate reader method | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750479 | Inhibition of PI3Kdelta (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1897592 | Inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation after 24 hrs by electrochemiluminescent assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID1897589 | Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID1897594 | Lipophilicity, logD of compound in 1-Octanol/PBS at pH 7.4 by LC-MS/MS method | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID1280830 | Selectivity index ratio of Kiapp for recombinant PI3K gamma (unknown origin) to Kiapp for PI3K alpha (unknown origin) using PIP2 as substrate | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1280872 | Decrease in phosphorylated Akt in nude mouse xenografted with human MCF7-neo/Her2 cells at 25 mg/kg administered as single dose after 1 hr by immunoassay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1280829 | Selectivity index ratio of Kiapp for recombinant PI3K delta (unknown origin) to Kiapp for PI3K alpha (unknown origin) using PIP2 as substrate | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750509 | Plasma clearance in nude mouse at 1 mg/kg, iv and 25 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750475 | Inhibition of DNA-dependent protein kinase (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280864 | Antitumor activity against human KPL4 cells xenografted in SCID beige mouse assessed as tumor growth inhibition at 25 mg/kg, po qd for 21 days | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750488 | Inhibition of PI3Kgamma (unknown origin) at 1 uM | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750469 | Plasma protein binding in human | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750489 | Inhibition of PI3Kdelta (unknown origin) at 1 uM | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750473 | Clearance in human hepatocytes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280839 | Volume of distribution at steady state in NCR nude mouse at 25 mg/kg, po | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1897603 | Inhibition of PI3Kdelta in human B-cells assessed as reduction in CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by flow cytometry analysis | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID750484 | Selectivity ratio of IC50 for human VPS34 to IC50 for PI3K alpha (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280854 | Plasma protein binding in CD-1 mouse at 5 uM after 4 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750511 | Intrinsic clearance in mouse liver microsomes after 1 hr by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280857 | Cytotoxicity against human KPL4 cells after 4 days by luminescence plate reader method | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750515 | Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750498 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 5.8 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750508 | Plasma protein binding in mouse by equilibrium dialysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750502 | Inhibition of PI3KC2beta (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1491596 | Inhibition of PI3K alpha (unknown origin) | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168). |
| AID1280858 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in mouse assessed as tumor growth inhibition at 25 mg/kg, po qd for 21 days | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750507 | Unbound clearance in nude mouse at 1 mg/kg, iv and 25 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750513 | Cytotoxicity against human MCF7-neo/Her2 cells after 3 to 4 days by CellTitre-Glo assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280876 | Toxicity in nude mouse xenografted with human MCF7-neo/Her2 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1897593 | Selectivity ratio of EC50 for PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation to EC50 for wild type PI3Kalpha in human HDQ-P1 cells assessed as reduction in PRAS40 phosphorylation | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID750487 | Inhibition of human VPS34 at 1 uM | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750483 | Plasma clearance in Sprague-Dawley rat | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750494 | Toxicity in nude mouse xenografted with human MCF7-neo/Her2 cells assessed as body weight loss relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750482 | Inhibition of PI3Kbeta (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1897604 | Selectivity ratio of IC90 for inhibition of PI3Kdelta in human B-cells assessed as reduction in CD69 expression to EC50 for inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID1491597 | Inhibition of PI3K delta (unknown origin) | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168). |
| AID750492 | In vivo inhibition of PI3Kalpha in human MCF7-neo/Her2 cells xenografted in nude mouse assessed as reduction in AKT phosphorylation at S473 at 2.8 mg/kg, po measured after 1 hr | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750497 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 2.8 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750477 | Cytotoxicity against human PC3 cells | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750472 | Clearance in mouse hepatocytes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750480 | Inhibition of PI3Kgamma (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750495 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 22.5 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750490 | Inhibition of PI3Kalpha (unknown origin) at 1 uM | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750470 | Plasma protein binding in rat | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280851 | Oral bioavailability in NCR nude mouse at 25 mg/kg | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID1280836 | Clearance in NCR nude mouse at 1 mg/kg, iv | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750481 | Oral bioavailability in Sprague-Dawley rat | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750474 | Inhibition of mTOR (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750496 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 11.25 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750476 | Inhibition of PI3KC2alpha (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750510 | Kinetic solubility of the compound | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750485 | Selectivity ratio of IC50 for PI3KC2 beta (unknown origin) to IC50 for PI3K alpha (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750478 | Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750471 | Clearance in rat hepatocytes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750506 | AUCtotal in nude mouse at 1 mg/kg, iv and 25 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750491 | Inhibition of PI3KC2beta (unknown origin) at 1 uM | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280875 | Toxicity in SCID beige mouse xenografted with human KPL4 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750514 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to apparent Ki for PI3K alpha (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1280847 | AUC in NCR nude mouse at 25 mg/kg, po | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750468 | Oral bioavailability in mouse | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1897591 | Selectivity ratio of Ki for PI3Kdelta (unknown origin) to Ki for PI3Kalpha (unknown origin) | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. |
| AID1280828 | Selectivity index ratio of Kiapp for recombinant PI3K beta (unknown origin) to Kiapp for PI3K alpha (unknown origin) using PIP2 as substrate | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide ( |
| AID750499 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 1.4 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID750505 | Unbound AUC in nude mouse at 1 mg/kg, iv and 25 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |