Detalles de la búsqueda
1.
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Bioorg Med Chem
; 29: 115865, 2021 01 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-33285410
2.
Interleukin 1/Toll-like receptor-induced autophosphorylation activates interleukin 1 receptor-associated kinase 4 and controls cytokine induction in a cell type-specific manner.
J Biol Chem
; 289(15): 10865-10875, 2014 Apr 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-24567333
3.
Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors.
Biochem J
; 460(2): 211-22, 2014 Jun 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-24593284
4.
Kinetic and structural characterization of DmpI from Helicobacter pylori and Archaeoglobus fulgidus, two 4-oxalocrotonate tautomerase family members.
Bioorg Chem
; 38(6): 252-9, 2010 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-20709352
5.
Activation loop phosphorylation modulates Bruton's tyrosine kinase (Btk) kinase domain activity.
Biochemistry
; 48(9): 2021-32, 2009 Mar 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-19206206
6.
Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820.
Structure
; 27(11): 1625-1633.e3, 2019 11 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-31693911
7.
3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
J Med Chem
; 62(15): 6876-6893, 2019 08 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-31282155
8.
Selling written-off A/R.
Healthc Financ Manage
; 62(9): 128-30, 132, 2008 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-18782990
9.
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
J Med Chem
; 61(23): 10665-10699, 2018 12 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-30423248
10.
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-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
J Med Chem
; 61(21): 9691-9721, 2018 11 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-30289716
11.
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
J Med Chem
; 60(5): 1971-1993, 2017 03 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-28139931
12.
Catalytically active MAP KAP kinase 2 structures in complex with staurosporine and ADP reveal differences with the autoinhibited enzyme.
Structure
; 11(6): 627-36, 2003 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-12791252
13.
A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Cancer Res
; 76(18): 5491-500, 2016 09 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27635045
14.
ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.
ACS Chem Biol
; 9(7): 1552-8, 2014 Jul 18.
Artículo
en Inglés
| MEDLINE | ID: mdl-24814050
15.
Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.
J Med Chem
; 55(22): 10047-63, 2012 Nov 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-23098091
16.
Identification and characterization of acidic mammalian chitinase inhibitors.
J Med Chem
; 53(16): 6122-8, 2010 Aug 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-20666458
17.
Triad of polar residues implicated in pH specificity of acidic mammalian chitinase.
Protein Sci
; 18(3): 569-78, 2009 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-19241384
18.
Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors.
J Med Chem
; 51(19): 5958-63, 2008 Oct 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-18783200
19.
Kinetic and stereochemical analysis of YwhB, a 4-oxalocrotonate tautomerase homologue in Bacillus subtilis: mechanistic implications for the YwhB- and 4-oxalocrotonate tautomerase-catalyzed reactions.
Biochemistry
; 46(42): 11919-29, 2007 Oct 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-17902707
20.
Inactivation of the phenylpyruvate tautomerase activity of macrophage migration inhibitory factor by 2-oxo-4-phenyl-3-butynoate.
Bioorg Chem
; 34(4): 183-99, 2006 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-16780921