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Isaac Hoffman

Observed names: Hoffman, Isaac, Hoffman, Isaac D., Hoffman, Isaac Dylan, I. Hoffman, I.D. Hoffman, Isaac D. Hoffman, Isaac Dylan Hoffman
Observed institution: Tyra Biosciences (United States)
ORCID: 0000-0003-2694-802X
Observed ORCID: 0000-0003-2694-802X
OpenAlex ID: A5017220522
Discovery of [cis-3-({(5R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
2018 · Mitsunori Kono, Atsuko Ochida, et al. · Journal of Medicinal Chemistry · 71
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
2017 · Tomohiro Okawa, Yoshio Aramaki, et al. · Journal of Medicinal Chemistry · 62
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)
2016 · Betty Lam, Yasuyoshi Arikawa, et al. · Bioorganic & Medicinal Chemistry Letters · 61
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A model for decoding resistance in precision oncology: acquired resistance to FGFR inhibitors in cholangiocarcinoma
2024 · L. Goyal, D. DiToro, et al. · Annals of Oncology · 50
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Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode
2019 · Jun Fujimoto, Osamu Kurasawa, et al. · ACS Medicinal Chemistry Letters · 40
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors
2006 · Leslie W. Tari, Isaac D. Hoffman, et al. · Bioorganic & Medicinal Chemistry Letters · 38
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders
2017 · Satoshi Mikami, Shinji Nakamura, et al. · Journal of Medicinal Chemistry · 36
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia
2024 · Robert L. Hudkins, Eric Allen, et al. · Journal of Medicinal Chemistry · 35
Mechanism of Inhibition of Novel Tryptophan Hydroxylase Inhibitors Revealed by Co-crystal Structures and Kinetic Analysis
2010 · Giovanni Cianchetta, Terry Stouch, et al. · Current Chemical Genomics · 35
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Assessment of the Target Engagement and d-Serine Biomarker Profiles of the d-Amino Acid Oxidase Inhibitors Sodium Benzoate and PGM030756
2017 · Eimear Howley, Michael Bestwick, et al. · Neurochemical Research · 30
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist
2019 · Tomoya Yukawa, Yoshi Nara, et al. · Journal of Medicinal Chemistry · 26
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
2017 · Yoshiyuki Fukase, Ayumu Sato, et al. · Bioorganic & Medicinal Chemistry · 26
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
2017 · Junya Shirai, Yoshihide Tomata, et al. · Bioorganic & Medicinal Chemistry · 24
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent
2020 · Osamu Kurasawa, Tohru Miyazaki, et al. · Journal of Medicinal Chemistry · 23
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones
2017 · Osamu Kurasawa, Yuya Oguro, et al. · Bioorganic & Medicinal Chemistry · 18
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors
2020 · Yusuke Sasaki, Hidekazu Tokuhara, et al. · Bioorganic & Medicinal Chemistry Letters · 17
Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders
2017 · Satoshi Mikami, Masanori Kawasaki, et al. · Chemical and Pharmaceutical Bulletin · 16
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Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate
2016 · Walter Keung, Amogh Boloor, et al. · Bioorganic & Medicinal Chemistry Letters · 15
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors
2009 · Theodore C. Jessop, James E. Tarver, et al. · Bioorganic & Medicinal Chemistry Letters · 11
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists
2019 · Ayumu Sato, Yoshiyuki Fukase, et al. · ChemMedChem · 8
Protein Crystallization for Structure-Based Drug Design
2011 · Isaac D. Hoffman · Methods in molecular biology · 7
TYRA-430: First reversible FGFR4/3 inhibitor designed to overcome current challenges in FGF19-driven hepatocellular carcinoma treatment.
2025 · Mohamed A. Ahmed, Jacqueline Starrett, et al. · Journal of Clinical Oncology · 2
Structure of RORgt in complex with a novel agonist.
2018 · R.J. Skene, I. Hoffman · Worldwide Protein Data Bank · 1
Structure-Based Design of a Novel Covalent 4-(1-Methylindol-3-yl)pyrimidin-2-amine Series Targeting FGFR2 Resistance Mutations
2026 · Robert L. Hudkins, Eric Allen, et al. · Journal of Medicinal Chemistry
CCDC 1918343: Experimental Crystal Structure Determination
2020 · Kurasawa, Osamu, Miyazaki, Tohru, et al. · The Cambridge Structural Database
Works count: 44
Citation count: 652
H-index: 16
I10-index: 19
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