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. |
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. |
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. |
AID1345671 | Human ATR serine/threonine kinase (ATR subfamily) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728379 | Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728349 | Growth inhibition of human LoVo cells after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1823236 | Upregulation of p21 protein expression in human HCT-116 cells at 10 uM measured after 20 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1823238 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1423077 | Inhibition of mTOR (unknown origin) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823222 | Binding affinity human TAF1 tandem bromodomain (1373 to 1499 residues) transfected in Escherichia coli BL21 (DE3) assessed as change in melting temperature by differential scanning fluorimetry | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1423083 | Cytotoxicity against human LoVo cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423090 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 25 mg/kg, po bid for 13 days and measured on day 22 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423065 | Inhibition of CYP2C19 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of NADPH by LC-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423055 | Inhibition of ATR in human HeLa cell nuclear extract using GST-fused p53N66 as substrate preincubated for 10 mins followed by ATP addition and measured after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423106 | Ratio of free plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 25 mg/kg, po bid to in vitro GI50 for human LoVo cells | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728354 | Inhibition of recombinant mTOR (unknown origin) assessed as residual activity at 1 uM | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1866068 | Inhibition of ATR (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
AID1652460 | Inhibition of 5'-TAMRA-labeled tracer 3',6'-bis(dimethylamino)-N-(4-{[2(1H-indol-4-yl)-6-(morpholin-4-yl)-pyrimidin-4-yl]amino}butyl)-3-oxo-3H-spiro[2-benzofuran-1,9'-xanthene]-5-carboxamide binding to recombinant human full-length N-terminal Flag-tagged | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. |
AID1823224 | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetric analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1823225 | Binding affinity to human TAF1 tandem bromodomain (1373 to 1499 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetric analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID728353 | Inhibition of PI3Kalpha (unknown origin) assessed as residual activity at 1 uM | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423061 | Fraction unbound in mouse 10% plasma | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728371 | Inhibition of human ERG by whole-cell electrophysiology assay | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423064 | Inhibition of CYP1A2 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of NADPH by LC-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423058 | Time dependent inhibition of CYP3A4 in human liver microsomes at 10 uM using midazolam as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 15 mins by LC-MS analysis relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823227 | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) by Alphascreen assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1423070 | Apparent permeability across apical to basolateral side in human Caco2 cells at 10 uM at pH 7.4 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423101 | Plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 25 mg/kg, po bid after 8 hrs | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728374 | Inhibition of mTOR-mediated AKT phosphorylation at serine 473 in human MDA-MB-468 cells | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423069 | Apparent permeability across apical to basolateral side in human Caco2 cells at 10 uM at pH 6.5 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423062 | Fraction unbound in human 10% plasma | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423081 | Inhibition of ATM phosphorylation at Ser1981 residue in human HT-29 cells using ionizing radiation | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423072 | Intrinsic clearance in human hepatocytes at 1 uM assessed per 10'6 cells | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823235 | Activation of p53 signaling pathway in human A549 cells assessed as p53 phosphorylation at S15 residue at 10 uM measured after 24 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID728358 | Inhibition of CYP1A2 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728378 | Inhibition of recombinant mTOR (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728347 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 13 days relative to control | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728364 | Aqueous solubility of the compound at pH 7.4 | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728362 | Oral bioavailability in Han-Wistar rat at 4 umol/kg | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423126 | Octanol-buffer partition co-efficient, log D of the compound at pH 7.4 by shake flask method | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823234 | Activation of p53 signaling pathway in human HCT-116 cells assessed as p53 phosphorylation at S15 residue at 10 uM measured after 20 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1866020 | Thermodynamic aqueous solubility of the compound | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
AID728357 | Inhibition of CYP2C9 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728355 | Inhibition of CYP2D6 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423088 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 14 days and measured on day 22 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728352 | Inhibition of PI3Kalpha-mediated AKT phosphorylation at threonine 308 in human BT474 cells | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728377 | Inhibition of PI3Kalpha (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423066 | Inhibition of CYP2C9 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of NADPH by LC-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728370 | Solubility of the compound in phosphate buffer after 24 hrs at pH 7.4 by LC-UV-MS analysis | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423056 | Inhibition of ATR in human HT29 cells after 60 mins by Hoechst 33258 staining-based assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423079 | Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in 70S6K S235/236 phosphorylation | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823243 | Induction of p53 accumulation in human A549 cells at 10 uM incubated for 24 hrs in presence of 10 Gy gamma irradiation by Western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID728346 | Toxicity in Swiss nu/nu mouse xenografted with human Lovo cells assessed as body weight loss at 25 mg/kg, po bid for 13 days | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423078 | Inhibition of mTOR in human MDA-MB-468 cells assessed as decrease in AKT phosphorylation at S473 residue | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823237 | Upregulation of p21 protein expression in human A549 cells at 10 uM measured after 24 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID1423086 | Toxicity in Swiss nu/nu mouse xenografted with human LoVo cells assessed as drug tolerability at 50 mg/kg, po qd administered via gavage | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423057 | Octanol-phosphate buffer partition co-efficient, log D of the compound at 10 uM at pH 7.4 after 3 hrs by shake flask method | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423082 | Inhibition of DNA-PK phosphorylation at Ser2056 residue in human HT-29 cells using ionizing radiation | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728372 | Octanol-buffer partition coefficient, log D of the compound at pH 7.4 by shake flask method | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728369 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM at pH 6.5 | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423087 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 20 days and measured on day 22 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728356 | Time dependent inhibition of CYP3A4-mediated midazolam metabolism in human liver microsomes at 10 uM by liquid chromatography-tandem mass spectrometry | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423071 | Intrinsic clearance in rat hepatocytes at 1 uM assessed per 10'6 cells | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423100 | Plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 50 mg/kg, po qd after 8 hrs | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423059 | Aqueous solubility in pH 7.4 phosphate buffer after 24 hrs by LC-UV-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728351 | Inhibition of ATM-mediated autophosphorylation at serine 1981 in human HT29 cells | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423080 | Inhibition of PI3Kalpha in human BT-474 cells assessed as decrease in AKT phosphorylation at T308 residue | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423084 | Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728375 | Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423089 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 13 days and measured on day 22 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728350 | Inhibition of DNA-PK-mediated autophosphorylation at serine 2056 in human HT29 cells | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423105 | Ratio of free plasma concentration in Swiss nu/nu mouse xenografted with human LoVo cells at 50 mg/kg, po qd to in vitro GI50 for human LoVo cells | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423068 | Inhibition of human ERG by whole cell electrophysiology analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1423067 | Inhibition of CYP2D6 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of NADPH by LC-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728345 | Toxicity in Swiss nu/nu mouse xenografted with human Lovo cells assessed as body weight loss at 50 mg/kg, po qd for 13 days | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728348 | Antitumor activity against human LoVo cells xenografted in Swiss nu/nu mouse assessed as tumor growth inhibition at 25 mg/kg, po bid for 13 days relative to control | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID728359 | Inhibition of CYP2C19 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423073 | Dose normalized AUC in Han-Wistar rat at 4 umol/kg, po | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID728368 | Intrinsic clearance in rat hepatocytes assessed per 10'6 cells at 1 uM | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1823223 | Binding affinity to human TAF1 BD 1 (1373 to 1499 residues) transfected in Escherichia coli BL21 (DE3) by isothermal titration calorimetric analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID728361 | Fraction unbound in rat plasma | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1423063 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of NADPH by LC-MS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
AID1823226 | Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by q-PCR based bromoscan assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
AID728360 | Inhibition of CYP3A4 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
AID1823221 | Binding affinity human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as change in melting temperature by differential scanning fluorimetry | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |