PMID

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Article Title

Organization

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved

Genentech

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.

Genentech

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Genentech

Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.

Genentech

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Genentech

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Genentech

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.

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Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

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The Rational Design of Selective Benzoxazepin Inhibitors of thea-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

Genentech

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Genentech

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.

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a-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.

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Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.

Genentech

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.

Genentech

Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.

Genentech

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.

Genentech

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.

Genentech

Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.

Genentech

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.

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Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.

Genentech

Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.

Genentech

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Genentech

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Genentech

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.

Genentech

Inhibiting the deubiquitinating enzymes (DUBs).

Genentech

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.

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Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Genentech

Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.

Genentech

Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.

Genentech

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Genentech

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.

Genentech

Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).

Genentech

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.

Genentech

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.

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Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.

Genentech

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

Genentech

Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.

Genentech

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Genentech

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

Genentech

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.

Genentech

Identification of tertiary sulfonamides as RORc inverse agonists.

Genentech

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.

Genentech

Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.

Genentech

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Genentech

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Genentech

Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Genentech

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.

Genentech

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Genentech

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.

Genentech

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

Genentech

Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Genentech

Lead identification of novel and selective TYK2 inhibitors.

Genentech

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

Genentech

Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Genentech

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.

Genentech

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Genentech

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Genentech

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Genentech

Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.

Genentech

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.

Genentech

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.

Genentech

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

Genentech

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Genentech

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

Genentech

Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Genentech

Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.

Genentech

Ras inhibition via direct Ras binding--is there a path forward?

Genentech

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.

Genentech

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Genentech

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Genentech

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Genentech

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea.

Genentech

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Genentech

Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

Genentech

Discovery of novel PI3-kinased specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

Genentech

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Genentech

Potent and selective inhibitors of PI3Kd: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Genentech

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Genentech

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.

Genentech

Inhibition of Wnt signaling by Dishevelled PDZ peptides.

Genentech

Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.

Genentech

Cyclic RGD peptide analogues as antiplatelet antithrombotics.

Genentech

N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship.

Genentech

Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.

Genentech

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

Genentech

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

Genentech

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Genentech

Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).

Genentech

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Genentech

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

Genentech

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

Genentech

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

Genentech

GDC-0449-a potent inhibitor of the hedgehog pathway.

Genentech

Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.

Genentech

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3K?.

Genentech

CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads.

Genentech

Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.

Genentech

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.

Genentech

Discovery of Acyl-sulfonamide Na

Genentech

Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Genentech

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3

Genentech

N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.

Genentech

A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists.

Genentech

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Genentech

Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.

Genentech

Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.

Genentech

Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.

Genentech

Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.

Genentech

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.

Genentech

Albumin affinity tags increase peptide half-life in vivo.

Genentech

Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.

Genentech

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Genentech

Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.

Genentech

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.

Genentech

Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.

Genentech

Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.

Genentech

Recent progress on nuclear receptor ROR? modulators.

Genentech

Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.

Genentech

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Genentech

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

Genentech

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Genentech

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.

Genentech

Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.

Genentech

Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.

Genentech

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.

Genentech

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na

Genentech

Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.

Genentech

Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.

Genentech

Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.

Genentech

Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.

Genentech

From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.

Genentech

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

Genentech

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.

Genentech

Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.

Genentech

Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).

Genentech

Na

Genentech

Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.

Genentech

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-?B Inducing Kinase.

Genentech

Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).

Genentech

Design of Selective Benzoxazepin PI3K? Inhibitors Through Control of Dihedral Angles.

Genentech

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

Genentech

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

Genentech

Structure-Based Design of Tricyclic NF-?B Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

Genentech

Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.

Genentech

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.

Genentech

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

Genentech

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

Genentech

Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.

Genentech

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

Genentech

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.

Genentech

Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor.

Genentech

Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.

Genentech

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

Genentech

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.

Genentech

Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.

Genentech

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists.

Genentech

A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.

Genentech

Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.

Genentech

A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.

Genentech

Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.

Genentech

A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.

Genentech