Human endogenous retrovirus-K (HERV-K) reverse transcriptase (RT) structure and biochemistry reveals remarkable similarities to HIV-1 RT and opportunities for HERV-K-specific inhibitionPROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICAIF9.12022-06-3022OAAI
Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's DiseaseJOURNAL OF MEDICINAL CHEMISTRYIF6.82021-03-309PRE
[1,2,4]Triazolo[1,5-a]pyrimidine Phosphodiesterase 2A Inhibitors: Structure and Free-Energy Perturbation-Guided ExplorationJOURNAL OF MEDICINAL CHEMISTRYIF6.82020-10-2713PREAI
Optimization of Potent and Selective Ataxia Telangiectasia-Mutated Inhibitors Suitable for a Proof-of-Concept Study in Huntington's Disease ModelsJOURNAL OF MEDICINAL CHEMISTRYIF6.82019-03-0619PREAI
Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary FibrosisJOURNAL OF MEDICINAL CHEMISTRYIF6.82017-05-01128OAAI
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)JOURNAL OF MEDICINAL CHEMISTRYIF6.82016-05-2330OAAI
Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class Ila Histone Deacetylase (HDAC) InhibitorsACS MEDICINAL CHEMISTRY LETTERSIF42015-12-2246OAAI
Lead Optimization toward Proof-of-Concept Tools for Huntington's Disease within a 4-(1H-Pyrazol-4-yl)pyrimidine Class of Pan-JNK InhibitorsJOURNAL OF MEDICINAL CHEMISTRYIF6.82015-03-1936PREAI
Design, Synthesis, and Biological Evaluation of Potent and Selective Class IIa Histone Deacetylase (HDAC) Inhibitors as a Potential Therapy for Huntington's DiseaseJOURNAL OF MEDICINAL CHEMISTRYIF6.82013-12-05134PREAI
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