标题
An Analysis of Successful Hit-to-Clinical Candidate Pairs
作者
关键词
-
出版物
Journal of Medicinal Chemistry
Volume 66, Issue 11, Pages 7101-7139
出版商
American Chemical Society (ACS)
发表日期
2023-05-25
DOI
10.1021/acs.jmedchem.3c00521
参考文献
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- Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1
- (2019) Sanjeev Kumar et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases
- (2019) Pamela A. Haile et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors
- (2019) Jian Lin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)
- (2019) Ryan Moslin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
- (2019) Stephen T. Wrobleski et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1S,2S)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma
- (2019) Magnus Munck af Rosenschöld et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies
- (2019) Harold G. Selnick et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer
- (2019) Shu-Yu Lin et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
- (2019) Yunhang Guo et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases
- (2019) Richard D. Caldwell et al. JOURNAL OF MEDICINAL CHEMISTRY
- Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor
- (2019) Junliang Hao et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)
- (2019) Carl A. Brooks et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC)
- (2019) Richard A. Ward et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer
- (2019) Youssef El-Ahmad et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
- (2019) Brian A. Lanman et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer
- (2019) Timo Heinrich et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor
- (2019) Frederick W. Goldberg et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure–Activity Relationship and Preclinical Characterization
- (2019) Neelima Sinha et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections
- (2019) Bin Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis
- (2018) Xueqing Wang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
- (2018) Christopher J. Helal et al. JOURNAL OF MEDICINAL CHEMISTRY
- Where Do Recent Small Molecule Clinical Development Candidates Come From?
- (2018) Dean G. Brown et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile
- (2018) Lena Ripa et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration
- (2018) Christopher M. Adams et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate
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- Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer
- (2018) George S. Tria et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development
- (2018) James J. Crawford et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation
- (2018) Brian T. O’Neill et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl
- (2018) RYO IWAMURA et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent
- (2018) Steven E. Van der Plas et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one)
- (2018) Kurt G. Pike et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
- (2018) Michael L. Vazquez et al. JOURNAL OF MEDICINAL CHEMISTRY
- Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism
- (2018) Yoshikazu Nishimura et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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 et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir
- (2018) Tao Wang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 (SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA)
- (2018) Hasane Ratni et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176)
- (2018) Alicia Regueiro-Ren et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1H,2H,3H-pyrrolo[3,2-b]pyridin-1-yl)-2-[(2R,5R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660)
- (2018) Christopher N. Johnson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders
- (2018) Justin S. Cisar et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of TRPM8 Antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine
- (2018) Daniel B. Horne et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
- (2018) Joseph Schoepfer et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis
- (2018) Panayiotis A. Procopiou et al. JOURNAL OF MEDICINAL CHEMISTRY
- Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)
- (2018) Hannah L. Woodward et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors
- (2018) Jason G. Kettle et al. JOURNAL OF MEDICINAL CHEMISTRY
- Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)
- (2018) Andrew Fensome et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Benzoazepinequinoline (BAQ) Derivatives as Novel, Potent, Orally Bioavailable Respiratory Syncytial Virus Fusion Inhibitors
- (2018) Xiufang Zheng et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis
- (2018) Michael G. Thomas et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent
- (2018) Kevin M. Foote et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)
- (2018) Atwood K. Cheung et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
- (2018) Paul M. Wehn et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Clinical Candidate 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor
- (2018) Kimiyuki Shibuya et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4)
- (2018) Edward J. Brnardic et al. JOURNAL OF MEDICINAL CHEMISTRY
- Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)-N-((S)-3-(Cyclopent-1-en-1-yl)-1-((R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propenamide)
- (2018) Henry W. B. Johnson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity
- (2018) Jay B. Fell et al. ACS Medicinal Chemistry Letters
- Design and Discovery of N-(2-Methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
- (2017) Gisele A. Nishiguchi et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
- (2017) Keith F. McDaniel et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
- (2017) Philip A. Harris et al. JOURNAL OF MEDICINAL CHEMISTRY
- Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach
- (2016) Paolo Innocenti et al. JOURNAL OF MEDICINAL CHEMISTRY
- Specific Correction of Alternative Survival Motor Neuron 2 Splicing by Small Molecules: Discovery of a Potential Novel Medicine To Treat Spinal Muscular Atrophy
- (2016) Hasane Ratni et al. JOURNAL OF MEDICINAL CHEMISTRY
- A phase I trial of the human double minute 2 inhibitor (MK-8242) in patients with refractory/recurrent acute myelogenous leukemia (AML)
- (2016) Farhad Ravandi et al. LEUKEMIA RESEARCH
- Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness
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- Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials
- (2016) T. G. Murali Dhar et al. ACS Medicinal Chemistry Letters
- Applications of Fluorine in Medicinal Chemistry
- (2015) Eric P. Gillis et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Early Clinical Development of 2-{6-[2-(3,5-Dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a Soft-Drug Inhibitor of Phosphodiesterase 4 for Topical Treatment of Atopic Dermatitis
- (2014) Jakob Felding et al. JOURNAL OF MEDICINAL CHEMISTRY
- Optimization of Potency and Pharmacokinetic Properties of Tetrahydroisoquinoline Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists
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- K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
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- Fused Piperidines as a Novel Class of Potent and Orally Available Transient Receptor Potential Melastatin Type 8 (TRPM8) Antagonists
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