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. |
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. |
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. |
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. |
AID1238682 | Inhibition of Mcl1 (unknown origin) assessed as inhibition of Mcl1-Bak interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238734 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 20 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238693 | Inhibition of cell proliferation of human Saos2 cells deficient with p53 gene | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238690 | Inhibition of cell proliferation of human HCT116 cells deficient with p53 gene | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238621 | Inhibition of cell proliferation of human SJSA1 cells | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238706 | Toxicity in monkey assessed as changes in testes parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238659 | Clearance in beagle dog at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238639 | AUC in Sprague-Dawley rat at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238702 | Toxicity in human SJSA1 cells xenografted dosed rat assessed as induction of histopathological changes at 30 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1555418 | Inhibition of p53 derived Cy5-p53 peptide (18 to 26 residues) binding to human MDM2 (2 to 188 residues) after 30 mins by TR-FRET assay | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy. |
AID1238635 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238680 | Inhibition of Bcl2 (unknown origin) assessed as inhibition of Bcl2-Bak interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238623 | Permeability of the compound by PAMPA method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238653 | Terminal half life in OF1 mouse at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238729 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 30 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238673 | Oral bioavailability in cynomolgus monkey at 0.3 mg/kg | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238652 | Volume of distribution at steady state in OF1 mouse at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238656 | Tmax in OF1 mouse at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238629 | Octanol water partition coefficient, logP of the compound | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238687 | Selectivity index, ratio of IC50 for Ras-Raf interaction (unknown origin) to IC50 for MDM2/p53 interaction (unknown origin) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1908067 | Inhibition of human MDM4 by TR-FRET assay | | | |
AID1238676 | Inhibition of human MDM2 L33E mutant (14 to 111 residues) by ITC method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238707 | Toxicity in rat assessed as changes in testes parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238642 | Oral bioavailability in Sprague-Dawley rat at 3 mg/kg | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238640 | Cmax in Sprague-Dawley rat at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238648 | Selectivity index, ratio of Ki for dog MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238739 | AUC (0 to 48 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 70 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238685 | Inhibition of cIAP (unknown origin) assessed as inhibition of cIAP-BIR3 interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238665 | Oral bioavailability in beagle dog at 0.3 mg/kg | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238683 | Inhibition of Mcl1 (unknown origin) assessed as inhibition of Mcl1-Noxa interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238668 | Volume of distribution at steady state in cynomolgus monkey at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238724 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 30 mg/kg, po dosed three times per week (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238712 | Toxicity in rat testes assessed as effect on proliferative cells | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238719 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as tumor regression at 70 mg/kg, po dosed three times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238649 | Selectivity index, ratio of Ki for mouse MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238696 | In-vivo inhibition of MDM2/p53 interaction in human SJSA1 cells xenografted rat assessed as increase in MDM2 mRNA level at 30 mg/kg, po measured within 72 hrs post dose by qRT-PCR method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238650 | Selectivity index, ratio of Ki for rat MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238681 | Inhibition of Bcl2 (unknown origin) assessed as inhibition of Bcl2-Bad interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238655 | Cmax in OF1 mouse at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238664 | Tmax in beagle dog at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238711 | Toxicity in rat assessed as induction of structural changes in testes tubular epithelium | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238695 | In-vivo inhibition of MDM2/p53 interaction in human SJSA1 cells xenografted rat assessed as increase in p21 mRNA level at 30 mg/kg, po measured within 72 hrs post dose by qRT-PCR method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238637 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238671 | Cmax in cynomolgus monkey at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238631 | Intrinsic clearance in human liver microsomes | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238732 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 5 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238645 | Inhibition of dog MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238698 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as reduction tumor growth dosed orally on daily basis under q24h regime | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238636 | Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238646 | Inhibition of mouse MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238733 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 10 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238738 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 70 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238667 | Clearance in cynomolgus monkey at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238670 | AUC in cynomolgus monkey at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238641 | Tmax in Sprague-Dawley rat at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238718 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as tumor regression at 30 mg/kg, po dosed three times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238663 | Cmax in beagle dog at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238678 | Potency index, ratio of IC50 for nutlin-3 to IC50 for test compound against human MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238675 | Inhibition of human MDM4 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238658 | Protein binding in OF1 mouse plasma by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238684 | Inhibition of XIAP (unknown origin) assessed as inhibition of XIAP-BIR3 interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238737 | AUC (0 to 48 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 30 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238677 | Binding affinity to human MDM2 assessed as change in melting temperature by DSF method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238703 | Toxicity in monkey assessed as changes in bone marrow parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238692 | Inhibition of cell proliferation of human SJSA1 cells expressing p53 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238628 | Time dependent inhibition of CYP3A4 in human liver microsomes | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238630 | Intrinsic clearance in monkey liver microsomes | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238715 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as effect on tumor growth at 10 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238647 | Inhibition of rat MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238662 | AUC in beagle dog at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238713 | Toxicity in monkey testes assessed as effect on germinal cells | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238735 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 30 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238721 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 10 mg/kg, po qd (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238704 | Toxicity in monkey assessed as changes in lymphoid organs parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238705 | Toxicity in monkey assessed as changes in GI tract parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238686 | Selectivity index, ratio of IC50 for p53-MDM4 (unknown origin) interaction to IC50 for MDM2/p53 interaction (unknown origin) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238730 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 30 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238727 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 10 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238714 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as effect on tumor growth at 5 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238691 | Selectivity index, ratio of IC50 for inhibition of cell proliferation of human HCT116 cells deficient with p53 gene to IC50 for inhibition of cell proliferation of human HCT116 cells expressing p53 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238722 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 20 mg/kg, po qd (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238657 | Oral bioavailability in OF1 mouse at 3 mg/kg | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238689 | Inhibition of cell proliferation of human HCT116 cells expressing p53 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238669 | Terminal half life in in cynomolgus monkey at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238716 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as effect on tumor growth at 20 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238694 | Selectivity index, ratio of IC50 for inhibition of cell proliferation of human Saos2 cells deficient with p53 gene to IC50 for inhibition of cell proliferation of human SJSA1 cells expressing p53 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238726 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 5 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238699 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as reduction tumor growth dosed orally three times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238725 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 70 mg/kg, po dosed three times per week (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1908066 | Inhibition of human MDM2 by TR-FRET assay | | | |
AID1238654 | AUC in OF1 mouse at 3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238688 | Inhibition of MDM2/p53 interaction (unknown origin) assessed as p53 nuclear translocation by GRIP p53 translocation assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238736 | AUC (0 to 24 hrs) in human SJSA1 cells xenografted rat assessed as mouse survival at 30 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238708 | Toxicity in rat assessed as changes in heart parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238660 | Volume of distribution at steady state in beagle dog at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238666 | Protein binding in beagle dog plasma by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238717 | Antitumor activity against human SJSA1 cells xenografted in rat assessed as tumor regression at 30 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238661 | Terminal half life in beagle dog at 0.1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238643 | Protein binding in Sprague-Dawley rat plasma by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238720 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 5 mg/kg, po qd (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238651 | Clearance in OF1 mouse at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238710 | Toxicity in female rat assessed as changes in adrenal gland parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238731 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 70 mg/kg, po dosed 3 times per week | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238728 | Toxicity in human SJSA1 cells xenografted rat assessed as mouse survival at 20 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238674 | Protein binding in cynomolgus monkey plasma by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238620 | Inhibition of MDM2/p53 interaction (unknown origin) using biotinylated MDM2 and Cy5-p53 (18 to 26 amino acids) by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238723 | Toxicity in human SJSA1 cells xenografted rat assessed as change in body weight at 30 mg/kg, po qd (Rvb = 1.9 to 6.8%) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238709 | Toxicity in male rat assessed as changes in adrenal gland parameters | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238679 | Inhibition of Ras (unknown origin) assessed as inhibition of Ras-Raf interaction by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238672 | Tmax in cynomolgus monkey at 0.3 mg/kg, po | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238701 | Toxicity in human SJSA1 cells xenografted dosed rat assessed as drug toleration dosed orally on daily basis under q24h regime | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238644 | Inhibition of human MDM2 by TR-FRET assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238700 | Toxicity in human SJSA1 cells xenografted dosed rat assessed as induction of histopathological changes dosed orally on daily basis under q24h regime | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
AID1238697 | In-vivo inhibition of MDM2/p53 interaction in human SJSA1 cells xenografted rat assessed as increase in PUMA mRNA level at 30 mg/kg, po measured within 72 hrs post dose by qRT-PCR method | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. |
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] |