Felix F Vajdos
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Explore the profile of Felix F Vajdos including associated specialties, affiliations and a list of published articles.
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852
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Recent Articles
1.
Schnute M, Trujillo J, Lee K, Unwalla R, Vajdos F, Kauppi B, et al.
ACS Med Chem Lett
. 2023 Feb;
14(2):191-198.
PMID: 36793423
Macrocyclic retinoic acid receptor-related orphan receptor C2 (RORC2) inverse agonists have been designed with favorable properties for topical administration. Inspired by the unanticipated bound conformation of an acyclic sulfonamide-based RORC2...
2.
Casimiro-Garcia A, Allais C, Brennan A, Choi C, Dower G, Farley K, et al.
J Med Chem
. 2021 Dec;
65(1):757-784.
PMID: 34967602
A diaryl ketone series was identified as vanin-1 inhibitors from a high-throughput screening campaign. While this novel scaffold provided valuable probe that was used to build target confidence, concerns over...
3.
Gerstenberger B, Ambler C, Arnold E, Banker M, Brown M, Clark J, et al.
J Med Chem
. 2020 Aug;
63(22):13561-13577.
PMID: 32787094
Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon family, where it...
4.
Gerstenberger B, Banker M, Clark J, Dowty M, Fensome A, Gifford R, et al.
Sci Rep
. 2020 Jun;
10(1):8974.
PMID: 32488071
Translation of modulation of drug target activity to therapeutic effect is a critical aspect for all drug discovery programs. In this work we describe the profiling of a non-receptor tyrosine-protein...
5.
Fensome A, Ambler C, Arnold E, Banker M, Clark J, Dowty M, et al.
Bioorg Med Chem
. 2020 Apr;
28(10):115481.
PMID: 32253095
Herein, we disclose a new series of TYK2/ JAK1 inhibitors based upon a 3.1.0 azabicyclic substituted pyrimidine scaffold. We illustrate the use of structure-based drug design for the initial design...
6.
Schnute M, Wennerstal M, Alley J, Bengtsson M, Blinn J, Bolten C, et al.
J Med Chem
. 2018 Aug;
61(23):10415-10439.
PMID: 30130103
The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of...
7.
Fensome A, Ambler C, Arnold E, Banker M, Brown M, Chrencik J, et al.
J Med Chem
. 2018 Aug;
61(19):8597-8612.
PMID: 30113844
Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway. JAK1 is important for the...
8.
Humphrey J, Movsesian M, Am Ende C, Becker S, Chappie T, Jenkinson S, et al.
J Med Chem
. 2018 May;
61(10):4635-4640.
PMID: 29718668
We disclose the discovery and X-ray cocrystal data of potent, selective quinazoline inhibitors of PDE1. Inhibitor ( S)-3 readily attains free plasma concentrations above PDE1 IC values and has restricted...
9.
Telliez J, Dowty M, Wang L, Jussif J, Lin T, Li L, et al.
ACS Chem Biol
. 2016 Oct;
11(12):3442-3451.
PMID: 27791347
PF-06651600, a newly discovered potent JAK3-selective inhibitor, is highly efficacious at inhibiting γc cytokine signaling, which is dependent on both JAK1 and JAK3. PF-06651600 allowed the comparison of JAK3-selective inhibition...
10.
Kung D, Griffith D, Esler W, Vajdos F, Mathiowetz A, Doran S, et al.
Bioorg Med Chem Lett
. 2015 Sep;
25(22):5352-6.
PMID: 26411795
A novel series of spirocyclic-diamine based, isoform non-selective inhibitors of acetyl-CoA carboxylase (ACC) is described. These spirodiamine derivatives were discovered by design of a library to mimic the structural rigidity...