Detalhe da pesquisa
1.
Metabolomic changes of the multi (-AGC-) kinase inhibitor AT13148 in cells, mice and patients are associated with NOS regulation.
Metabolomics
; 16(4): 50, 2020 04 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-32285223
2.
Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution.
Xenobiotica
; 47(9): 771-777, 2017 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-27618572
3.
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies.
J Med Chem
; 66(8): 5907-5936, 2023 04 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-37017629
4.
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones.
J Med Chem
; 66(8): 5892-5906, 2023 04 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-37026591
5.
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo.
J Med Chem
; 65(12): 8191-8207, 2022 06 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-35653645
6.
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
J Med Chem
; 65(12): 8169-8190, 2022 06 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-35657291
7.
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket.
J Med Chem
; 64(23): 17079-17097, 2021 12 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-34846884
8.
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.
J Med Chem
; 63(8): 4047-4068, 2020 04 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-32275432
9.
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-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
J Med Chem
; 61(18): 8226-8240, 2018 09 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-30199249
10.
Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma.
Mol Cancer Ther
; 16(10): 2315-2323, 2017 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-28637716
11.
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
J Med Chem
; 60(1): 180-201, 2017 01 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-28004573
12.
Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation.
Mol Cancer Ther
; 15(6): 1412-24, 2016 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-27048952
13.
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
J Med Chem
; 59(8): 3671-88, 2016 04 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-27055065
14.
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Oncotarget
; 7(3): 2329-42, 2016 Jan 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-26295308
15.
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.
Medchemcomm
; 7(8): 1580-1586, 2016 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27746890
16.
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
J Med Chem
; 59(11): 5221-37, 2016 06 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-27167172
17.
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
J Med Chem
; 58(4): 1717-35, 2015 Feb 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-25680029
18.
Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.
Mol Cancer Ther
; 8(7): 1725-38, 2009 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-19584227