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287 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an ImprovedEBI
Genentech
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.EBI
Genentech
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.EBI
Genentech
Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.EBI
Genentech
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.EBI
Genentech
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.EBI
Genentech
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.EBI
Genentech
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.EBI
Genentech
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).EBI
Genentech
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.EBI
Genentech
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.EBI
Genentech
a-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.EBI
Genentech
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.EBI
Genentech
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.EBI
Genentech
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.EBI
Genentech
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.EBI
Genentech
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.EBI
Genentech
Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.EBI
Genentech
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.EBI
Genentech
Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.EBI
Genentech
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.EBI
Genentech
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.EBI
Genentech
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.EBI
Genentech
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.EBI
Genentech
Inhibiting the deubiquitinating enzymes (DUBs).EBI
Genentech
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.EBI
Genentech
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.EBI
Genentech
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.EBI
Genentech
Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.EBI
Genentech
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.EBI
Genentech
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.EBI
Genentech
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).EBI
Genentech
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.EBI
Genentech
Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.EBI
Genentech
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.EBI
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.EBI
Genentech
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.EBI
Genentech
Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.EBI
Genentech
Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.EBI
Genentech
Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.EBI
Genentech
Identification of tertiary sulfonamides as RORc inverse agonists.EBI
Genentech
Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.EBI
Genentech
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.EBI
Genentech
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).EBI
Genentech
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.EBI
Genentech
Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).EBI
Genentech
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.EBI
Genentech
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.EBI
Genentech
Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.EBI
Genentech
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.EBI
Genentech
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).EBI
Genentech
Lead identification of novel and selective TYK2 inhibitors.EBI
Genentech
2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.EBI
Genentech
Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.EBI
Genentech
Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.EBI
Genentech
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.EBI
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.EBI
Genentech
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.EBI
Genentech
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.EBI
Genentech
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.EBI
Genentech
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.EBI
Genentech
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).EBI
Genentech
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.EBI
Genentech
Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.EBI
Genentech
Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.EBI
Genentech
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.EBI
Genentech
Ras inhibition via direct Ras binding--is there a path forward?EBI
Genentech
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.EBI
Genentech
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.EBI
Genentech
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI
Genentech
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.EBI
Genentech
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea.EBI
Genentech
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.EBI
Genentech
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.EBI
Genentech
Discovery of novel PI3-kinased specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.EBI
Genentech
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.EBI
Genentech
Potent and selective inhibitors of PI3Kd: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.EBI
Genentech
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).EBI
Genentech
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.EBI
Genentech
Inhibition of Wnt signaling by Dishevelled PDZ peptides.EBI
Genentech
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.EBI
Genentech
Cyclic RGD peptide analogues as antiplatelet antithrombotics.EBI
Genentech
N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship.EBI
Genentech
Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.EBI
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.EBI
Genentech
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.EBI
Genentech
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.EBI
Genentech
Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).EBI
Genentech
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.EBI
Genentech
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.EBI
Genentech
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.EBI
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.EBI
Genentech
GDC-0449-a potent inhibitor of the hedgehog pathway.EBI
Genentech
Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.EBI
Genentech
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).EBI
Genentech
GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1.EBI
Genentech
Structure-Based Design and Evaluation of Reversible KRAS G13D Inhibitors.EBI
Genentech
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.EBI
Genentech
Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs.EBI
Genentech
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.EBI
Genentech
It's ok to be outnumbered - sub-stoichiometric modulation of homomeric protein complexes.EBI
Genentech
Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer.EBI
Genentech
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.EBI
Genentech
CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads.EBI
Genentech
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.EBI
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.EBI
Genentech
Discovery of Acyl-sulfonamide NaEBI
Genentech
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).EBI
Genentech
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3EBI
Genentech
N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.EBI
Genentech
A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists.EBI
Genentech
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.EBI
Genentech
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.EBI
Genentech
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.EBI
Genentech
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.EBI
Genentech
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.EBI
Genentech
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.EBI
Genentech
Albumin affinity tags increase peptide half-life in vivo.EBI
Genentech
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.EBI
Genentech
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.EBI
Genentech
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.EBI
Genentech
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.EBI
Genentech
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.EBI
Genentech
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.EBI
Genentech
Recent progress on nuclear receptor RORγ modulators.EBI
Genentech
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.EBI
Genentech
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.EBI
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.EBI
Genentech
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.EBI
Genentech
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.EBI
Genentech
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.EBI
Genentech
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.EBI
Genentech
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.EBI
Genentech
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide NaEBI
Genentech
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.EBI
Genentech
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.EBI
Genentech
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.EBI
Genentech
Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.EBI
Genentech
From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.EBI
Genentech
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.EBI
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.EBI
Genentech
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.EBI
Genentech
Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).EBI
Genentech
NaEBI
Genentech
Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.EBI
Genentech
Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.EBI
Genentech
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).EBI
Genentech
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.EBI
Genentech
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).EBI
Genentech
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).EBI
Genentech
Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).EBI
Genentech
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.EBI
Genentech
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.EBI
Genentech
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.EBI
Genentech
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.EBI
Genentech
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.EBI
Genentech
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.EBI
Genentech
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.EBI
Genentech
Compounds for the treatment of respiratory diseasesBDB
University of Melbourne
HETEROCYCLIC AGONISTSBDB
Gasherbrum Bio
PYRROLO[1,2-b]-2-PYRIDAZINONE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTSBDB
Suven Life Sciences
COMPOUND OF THE 7A,8,9,10,11,11A-HEXAHYDRO-1H,7H-PYRANO[2,3-C]XANTHENE TYPE, METHOD OF PREPARATION THEREOF, INTERMEDIATES THEREOF AND THERAPEUTIC APPLICATIONS THEREOFBDB
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE; INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE; UNIVERSITÉ CÔTE D''AZUR
AROMATIC ACETYLENE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOFBDB
Zhejiang Hisun Pharmaceutical
PRMT5 INHIBITOR AND THE USE THEREOFBDB
Cytosinlab Therapeutics
ISOXAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERED RELATED THERETOBDB
Arena Pharmaceuticals
TYK2 INHIBITORSBDB
Biogen Ma
PYRAZOLYL DERIVATIVES AS INHIBITORS OF THE KRAS MUTANT PROTEINBDB
Novartis
FUSED TRI-CYCLIC COMPOUND AS A PDE3/PDE4 DUAL INHIBITORBDB
Chia Tai Tianqing Pharmaceutical Group
DUAL WNT SIGNALING PATHWAY INHIBITORS AND AMPK ACTIVATORS FOR TREATMENTS OF DISEASEBDB
University of Maryland at Baltimore
Iminosulfanone compound as bromodomain protein inhibitor and pharmaceutical composition and medical use thereofBDB
Chia Tai Tianqing Pharmaceutical Group
KRAS INHIBITORSBDB
Bristol-Myers Squibb
Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)BDB
Incyte
COMPOUND HAVING INHIBITORY ACTIVITY AGAINST O-GLUSACASE AND USE THEREOFBDB
Medifron Dbt
UNIT DOSAGE COMPOSITION OF AKT INHIBITORBDB
Nanjing Chia Tai Tianqing Pharmaceutical
Benzenesulfonylbenazamide compound for inhibiting BCL-2 protein and composition and use thereofBDB
Shenzhen Targetrx
Compounds for degrading Tau protein aggregates and uses thereofBDB
Aprinoia Therapeutics
Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disordersBDB
Mindset Pharma
Bicyclic heterocycles as FGFR inhibitorsBDB
Incyte
ACLY inhibitors and uses thereofBDB
Nimbus Artemis
Substituted quinolines useful as kinase inhibitorsBDB
Teligene
Melt-extruded solid dispersions containing an apoptosis-inducing agentBDB
Abbvie
Protease inhibitorsBDB
Medivir
Pyrazole compoundBDB
Sumitomo Dainippon Pharma
Piperidin-4-yl azetidine derivatives as JAK1 inhibitorsBDB
Incyte
Formulations of an AXL/MER inhibitorBDB
Incyte
Aminobenzimidazole derivatives, treatments, and methods of inhibiting histone deacetylaseBDB
Translational Drug Development
Heterocycles useful as anti-cancer agentsBDB
Hangzhou Innogate Pharma
Substituted pyridines as inhibitors of histone deacetylaseBDB
Alkermes
Indane-amines as PD-L1 antagonistsBDB
Chemocentryx
Crystal form of urate transporter 1 inhibitor and preparation method and use thereofBDB
Tianjin Institute of Pharmaceutical Research
Aryl-or heteroaryl-substituted benzene compoundsBDB
Epizyme
6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives as PDE3A and PDE3B inhibitors for treating cancerBDB
Bayer Aktiengesellschaft
Fused heterocyclic derivatives, their preparation methods thereof and medical uses thereofBDB
Beijing Innocare Pharma Tech
Piperazinyl norbenzomorphan compounds and methods for using the sameBDB
University Of Texas
Therapeutic compounds and methods of use thereofBDB
Genentech
Inhibitors of lysine specific demethylase-1BDB
Celgene Quanticel Research
Therapeutic inhibitory compoundsBDB
Attune Pharmaceuticals
Compound useful for the treatment of degenerative and inflammatory diseasesBDB
Galapagos
Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activityBDB
Astex Therapeutics
Benzothiophene estrogen receptor modulatorsBDB
G1 Therapeutics
Therapeutically active compounds and their methods of useBDB
Agios Pharmaceuticals
Treatment and diagnosis of melanomaBDB
Rockefeller University
Kinase inhibitorsBDB
Oxular Acquisitions
IRAK4 modulatorsBDB
Genentech
Heteroarylbenzimidazole compoundsBDB
Bayer Pharma Aktiengesellschaft
Modulators of P97 AAA ATPase activityBDB
University of Pittsburgh
Inhibitors of phosphatidylinositol 3-kinase gammaBDB
Astrazeneca
Substituted dihydropyrazino[1 ′,2′:1,5]pyrrolo[2,3-d]pyrimidine-based antiproliferative agentsBDB
Gi Therapeutics
Neprilysin inhibitorsBDB
Theravance Biopharma R&D Ip
Compounds that are ERK inhibitorsBDB
Merck Sharp & Dohme
GLP-1 receptor agonists and uses thereofBDB
Pfizer
Indazole amine derivative, preparation method therefor and medical use thereofBDB
Zhejiang Hisun Pharmaceutical
Quinoxaline compounds as type III receptor tyrosine kinase inhibitorsBDB
Development Center For Biotechnology
Heterocyclic compounds used as FGFR inhibitorsBDB
Nanjing Innocare Pharma Tech
4-(biphen-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I) as GABA receptor modulators for use in the treatment of epilepsy and painBDB
Pfizer
Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activityBDB
Northwestern University
BCL-2 inhibitorsBDB
Newave Pharmaceutical
Bipyrazole derivatives as JAK inhibitorsBDB
Incyte
Compounds useful as inhibitors of ATR kinaseBDB
Vertex Pharmaceuticals
Benzoxazinone amides as mineralocorticoid receptor modulatorsBDB
Astrazeneca
Benzimidazole derivatives as bromodomain inhibitorsBDB
Gilead Sciences
Tricyclic compounds as anticancer agentsBDB
Bristol-Myers Squibb
Pyridine compounds used as PI3 kinase inhibitorsBDB
Teligene
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitorsBDB
Vtv Therapeutics
Biochemical characterization of the chloroplastic ß-carbonic anhydrase from Flaveria bidentis (L.) "Kuntze".BDB
Istituto Di Biostrutture E Bioimmagini-Cnr
Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.BDB
Nas of Ukraine
Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII.BDB
Vilnius University
Combination therapy for treating cancerBDB
Epizyme
Selective histone deactylase 6 inhibitorsBDB
H. Lee Moffitt Cancer Center and Research Institute
Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compoundsBDB
Pfizer
Carboxamide derivativesBDB
Novartis
Triazolopyrazine derivative and use thereofBDB
Korea Research Institute of Chemical Technology
Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions.BDB
Chulalongkorn University
Urease inhibitors from Hypericum oblongifolium WALL.BDB
University of Peshawar
Potent inhibitory effects of benzyl and p-xylidine-bis dithiocarbamate sodium salts on activities of mushroom tyrosinase.BDB
University of Tehran
Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.BDB
Medical University of Bialystok
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.BDB
Dublin City University
Validation of flavonoids as potential dipeptidyl peptidase III inhibitors: Experimental and computational approach.BDB
Josip Juraj Strossmayer University of Osijek
Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor.BDB
Jamia Hamdard (Hamdard University)
Synthesis, molecular docking studies of hybrid benzimidazole as a-glucosidase inhibitor.BDB
Universiti Teknologi Mara (Uitm)
Inhibitors of bruton's tyrosine kinase for the treatment of solid tumorsBDB
Pharmacyclics
Perfluoro-tert-butyl Homoserine Is a Helix-Promoting, Highly Fluorinated, NMR-Sensitive Aliphatic Amino Acid: Detection of the Estrogen Receptor·Coactivator Protein-Protein Interaction by (19)F NMR.BDB
University of Delaware
The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.BDB
Soochow University
Chemical compoundsBDB
Astrazeneca
Kinase inhibitorsBDB
Allergan
Coumarin-thiazole and -oxadiazole derivatives: Synthesis, bioactivity and docking studies for aldose/aldehyde reductase inhibitors.BDB
Comsats Institute of Information Technology
In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase.BDB
Universiti Teknologi Mara (Uitm)
5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2.BDB
Bharati Vidyapeeth'S College of Pharmacy
Quinazoline-7-ether compounds and methods of useBDB
Newgen Therapeutics
Indolinone protein kinase inhibitorsBDB
Beta Pharma
Dissecting the Multiple Roles of PqsE in Pseudomonas aeruginosa Virulence by Discovery of Small Tool Compounds.BDB
Helmholtz-Institute For Pharmaceutical Research Saarland
Design, synthesis and antitumor activity of novel pyrazolo[3,4-d]pyrimidine derivatives as EGFR-TK inhibitors.BDB
Beni-Suef University
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseasesBDB
Galderma Research & Development
Novel 4-heteroaryl-antipyrines as DPP-IV inhibitors.BDB
Cairo University
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.BDB
University of Wisconsin-Madison
Sulfamide sodium channel inhibitorsBDB
Amgen
IRE-1α inhibitorsBDB
Mannkind
Compounds and methods useful for directing stem cell differentiationBDB
Vanderbilt University
Chemical compoundsBDB
Astrazeneca
Monocyclic pyridine derivativeBDB
Eisai R&D Management
Pyrazolopyrimidine JAK inhibitor compounds and methodsBDB
Genentech
Pyrrolidine derivativesBDB
Hoffmann-La Roche
Uracil compound or salt thereof having human deoxyuridine triphosphatase inhibitory activityBDB
Taiho Pharmaceutical
Glucagon receptor modulatorsBDB
Pfizer
Imidazo[1,2-B][1,2,4]triazines as C-MET inhibitorsBDB
Incyte
Dehydroquinate synthase: the use of substrate analogues to probe the late steps of the catalyzed reaction.BDB
Harvard University
Interaction of flexible analogs of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and of N-methyl-4-phenylpyridinium with highly purified monoamine oxidase A and B.BDB
University of California San Francisco
Acyclic Immucillin Phosphonates: Second-Generation Inhibitors of Plasmodium falciparum Hypoxanthine- Guanine-Xanthine Phosphoribosyltransferase.BDB
Albert Einstein College of Medicine
Synthesis and biological evaluation of some new N(4)-substituted isatin-3-thiosemicarbazones.BDB
Bahauddin Zakariya University
In silico studies of urease inhibitors to explore ligand-enzyme interactions.BDB
Quaid-I-Azam University
Kinetic properties and inhibition of the dimeric dUTPase-dUDPase from Campylobacter jejuni.BDB
Instituto De Parastiologia Y Biomedicina "Lopez-Neyra
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.BDB
Case Western Reserve University
Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.BDB
UniversitÀ
Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor.BDB
University of Turku
Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.BDB
Glaxo Group Research
Amplification of the rat M2 muscarinic receptor gene by the polymerase chain reaction: functional expression of the M2 muscarinic receptor.BDB
University of Arizona
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitorsBDB
Array Biopharma
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity.BDB
University of Oxford
Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group.BDB
Tohoku College of Pharmacy
Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.BDB
Parke-Davis Pharmaceutical Research