64 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
The Institute of Cancer Research
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
The Institute of Cancer Research
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.
The Institute of Cancer Research
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
The Institute of Cancer Research
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
The Institute of Cancer Research
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
The Institute of Cancer Research
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
The Institute of Cancer Research
Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines.
The Institute of Cancer Research
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).
The Institute of Cancer Research
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.
The Institute of Cancer Research
Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.
The Institute of Cancer Research
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.
The Institute of Cancer Research
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
The Institute of Cancer Research
Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
The Institute of Cancer Research
Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).
The Institute of Cancer Research
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
The Institute of Cancer Research
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.
The Institute of Cancer Research
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
The Institute of Cancer Research
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
The Institute of Cancer Research
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.
The Institute of Cancer Research
Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2.
The Institute of Cancer Research
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
The Institute of Cancer Research
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
The Institute of Cancer Research
Molecular modeling studies on G-quadruplex complexes of telomerase inhibitors: structure-activity relationships.
The Institute of Cancer Research
2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase.
The Institute of Cancer Research
1,4- and 2,6-disubstituted amidoanthracene-9,10-dione derivatives as inhibitors of human telomerase.
The Institute of Cancer Research
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
The Institute of Cancer Research
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.
The Institute of Cancer Research
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute of Cancer Research
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.
The Institute of Cancer Research
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
The Institute of Cancer Research
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.
The Institute of Cancer Research
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.
The Institute of Cancer Research
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
The Institute of Cancer Research
Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).
The Institute of Cancer Research
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute of Cancer Research
The identification of novel PLC-gamma inhibitors using virtual high throughput screening.
The Institute of Cancer Research
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.
The Institute of Cancer Research
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6
The Institute of Cancer Research
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
The Institute of Cancer Research
Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.
The Institute of Cancer Research
The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.
The Institute of Cancer Research
Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).
The Institute of Cancer Research
Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72.
The Institute of Cancer Research
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
The Institute of Cancer Research
Human telomerase inhibition by substituted acridine derivatives.
The Institute of Cancer Research
Human telomerase inhibition by regioisomeric disubstituted amidoanthracene-9,10-diones.
The Institute of Cancer Research
Privileged Structures and Polypharmacology within and between Protein Families.
The Institute of Cancer Research
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.
The Institute of Cancer Research
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
The Institute of Cancer Research
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
The Institute of Cancer Research
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
The Institute of Cancer Research
Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.
The Institute of Cancer Research
Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.
The Institute of Cancer Research
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.
The Institute of Cancer Research
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 N
The Institute of Cancer Research
Process for preparing a compound useful for producing an optically active diazabicyclooctane compound
Meiji Seika Pharma