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Title: Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1900857
Journal Information:
J. Med. Chem., Vol. 65, Issue (15)
Country of Publication:
United States
Language:
ENGLISH

References (40)

Cyclin E1 and cyclin-dependent kinase 2 are critical for initiation, but not for progression of hepatocellular carcinoma journal August 2018
Regulation of G2/M Transition by Inhibition of WEE1 and PKMYT1 Kinases journal November 2017
CCNE1 copy number is a biomarker for response to combination WEE1-ATR inhibition in ovarian and endometrial cancer models journal September 2021
The CDK1 inhibitory kinase MYT1 in DNA damage checkpoint recovery journal November 2012
CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition journal April 2022
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma journal July 2021
Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells journal February 2011
Use of Kinase Inhibitors to Correct ΔF508-CFTR Function journal September 2012
ADP-Glo: A Bioluminescent and Homogeneous ADP Monitoring Assay for Kinases journal December 2009
2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of N -(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a Potent pan -Src Kinase Inhibitor journal November 2006
Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity journal October 2001
Pyrrolo[3,2-b]quinoxaline Derivatives as Types I1/2 and II Eph Tyrosine Kinase Inhibitors: Structure-Based Design, Synthesis, and in Vivo Validation journal July 2014
Hydrogen Bonding Penalty upon Ligand Binding journal June 2011
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics journal August 2007
Understanding substrate selectivity of human UDP-glucuronosyltransferases through QSAR modeling and analysis of homologous enzymes journal March 2012
AlphaLISA immunoassays: the no-wash alternative to ELISAs for research and drug discovery journal December 2008
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement journal February 2018
Assessing Atropisomer Axial Chirality in Drug Discovery and Development journal September 2011
Functional Interrogation of the Kinome Using Nucleotide Acyl Phosphates journal January 2007
An Azo Coupling Strategy for Protein 3‐Nitrotyrosine Derivatization journal August 2019
DDX3X inhibitors, an effective way to overcome HIV-1 resistance targeting host proteins journal August 2020
Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions journal September 2016
Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach journal March 2021
Efficient Pd-catalyzed domino synthesis of 1-phenyl-1H-indol-2-amine and 5-amino-indolo[1,2-a]quinazoline derivatives journal January 2015
Boron Trichloride/Tetra-n-Butylammonium Iodide:  A Mild, Selective Combination Reagent for the Cleavage of Primary Alkyl Aryl Ethers journal November 1999
A new homogeneous platinum containing catalyst for the hydrolysis of nitriles journal November 1995
Studies on pyrimidine derivatives. XXI. Nucleophilic substitution of 4-chloropyrimidines and related compounds with carbanions. journal January 1981
A Convenient Protocol for the Synthesis of Hindered Aryl Malononitriles journal November 2006
Binding Mode of an α-Amino Acid-Linked Quinoxaline-2,3-dione Analogue at Glutamate Receptor Subtype GluK1 journal April 2015
Synthesis of (±)-14-epi-hydroxydolasta-1(15),7,9-triene and (±)-7-epi-acetoxy-14-epi-hydroxydolasta-1(15),8-diene*Taken in part from the Ph.D. dissertation of Jianhua Yu, University of Georgia, Athens, Georgia, USA, 2009. journal January 2012
Cyanation of aromatic halides journal August 1987
Palladium-Catalyzed Cross-Coupling Reactions of Organoboron Compounds journal November 1995
Alkyl nitrite-metal halide deamination reactions. 2. Substitutive deamination of arylamines by alkyl nitrites and copper(II) halides. A direct and remarkably efficient conversion of arylamines to aryl halides journal July 1977
Reduction of animal usage by serial bleeding of mice for pharmacokinetic studies: application of robotic sample preparation and fast liquid chromatography–mass spectrometry journal April 2001
XDS journal January 2010
Phaser crystallographic software journal July 2007
The Phenix software for automated determination of macromolecular structures journal September 2011
Features and development of Coot journal March 2010
Collaboration gets the most out of software journal September 2013
Synthesis and Some Reactions of 3-Chloro-2-(cyanomethylene)-1,2-dihydroquinoxalines journal March 2004