Detalles de la búsqueda
1.
Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived ß 2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.
J Pharmacol Exp Ther
; 369(2): 188-199, 2019 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-30819762
2.
Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human ß2 Adrenoceptor.
Mol Pharmacol
; 89(4): 467-75, 2016 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-26772612
3.
Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.
Bioorg Med Chem Lett
; 26(19): 4729-4734, 2016 10 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27575470
4.
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Bioorg Med Chem Lett
; 26(8): 2057-64, 2016 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26951753
5.
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
Bioorg Med Chem Lett
; 25(17): 3582-4, 2015 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26164189
6.
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Bioorg Med Chem Lett
; 25(17): 3575-81, 2015 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26199119
7.
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Bioorg Med Chem Lett
; 25(17): 3569-74, 2015 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26206504
8.
Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the ß2-adrenoceptor.
Mol Pharmacol
; 85(4): 608-17, 2014 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-24476583
9.
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting ß2-adrenoceptor agonist.
Bioorg Med Chem Lett
; 24(17): 4341-7, 2014 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25065493
10.
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Bioorg Med Chem Lett
; 23(13): 3741-8, 2013 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23726034
11.
An investigation into the structure-activity relationships associated with the systematic modification of the ß(2)-adrenoceptor agonist indacaterol.
Bioorg Med Chem Lett
; 22(19): 6280-5, 2012 Oct 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-22932315
12.
Exploring the kinetic selectivity of drugs targeting the ß1 -adrenoceptor.
Pharmacol Res Perspect
; 10(4): e00978, 2022 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-35762357
13.
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
J Med Chem
; 65(12): 8345-8379, 2022 06 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-35500094
14.
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
Bioorg Med Chem Lett
; 20(17): 5302-7, 2010 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-20655218
15.
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Bioorg Med Chem Lett
; 20(3): 1219-24, 2010 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-20031406
16.
Correction to "2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4".
ACS Med Chem Lett
; 11(11): 2341, 2020 Nov 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-33214851
17.
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
J Med Chem
; 63(21): 12542-12573, 2020 11 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-32930584
18.
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Bioorg Med Chem Lett
; 19(16): 4794-8, 2009 Aug 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19592244
19.
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Mol Cancer Ther
; 18(12): 2194-2206, 2019 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-31409633
20.
2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.
ACS Med Chem Lett
; 9(3): 215-220, 2018 Mar 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-29541363