A. Thorarensen

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Aliases
A Thorarensen, A. Thorarensen, Atli Thorarensen
Publication record
80 papers · 2,483 citations · H-index 27

PAPERS

Discovery of PF-07054894, a Potent Squaramide-Based CCR6 Antagonist Displaying High CXCR2 Selectivity.
20251 citationsauthor #45
Conformational Role of Methyl in the Potency of Cyclohexane-Substituted Squaramide CCR6 Antagonists.
20258 citationsauthor #20
Understanding CXCR2 antagonism with a dynamic allosteric ternary complex model.
20240 citationsauthor #4
Structural basis for CCR6 modulation by allosteric antagonists
202411 citationsauthor #34
A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6+ T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation
202316 citationsauthor #20
Meet Our Associate Editor
20200 citationsauthor #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.
202045 citationsauthor #1
PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor.
2019129 citationsauthor #12
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
201830 citationsauthor #58
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
201858 citationsauthor #21
Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells.
201727 citationsauthor #12
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.
2017133 citationsauthor #1
Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms
201737 citationsauthor #9
CCDC 1536276: Experimental Crystal Structure Determination
20170 citationsauthor #1
Target the More Druggable Protein States in a Highly Dynamic Protein-Protein Interaction System
201613 citationsauthor #2
Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free‐Energy Perturbation (FEP)
201640 citationsauthor #17
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
201643 citationsauthor #28
Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide
201644 citationsauthor #20
OP0155 Development of A JAK3 Specific Inhibitor Clinical Candidate: Functional Differentiation of JAK3 Selective Inhibition over PAN-JAK or JAK1 Selective Inhibition
20160 citationsauthor #15
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.
2016166 citationsauthor #36
New spleen tyrosine kinase inhibitors: patent applications published during 2011-2013.
20148 citationsauthor #1
ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.
201457 citationsauthor #1
Crystal structure of hH-PGDS with water displacing inhibitor
20120 citationsauthor #2
CHAPTER 7:Syk Kinase Inhibitors
20120 citationsauthor #3
The 2010 patent landscape for spleen tyrosine kinase inhibitors.
201214 citationsauthor #5
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters.
201222 citationsauthor #14
Identification of Type‐II Inhibitors Using Kinase Structures
201224 citationsauthor #14
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.
201128 citationsauthor #16
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds.
201120 citationsauthor #14
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
201022 citationsauthor #35
An Efficient and RegioselectiveDifluoromethylation of 3-Iodoindazole with Chlorodifluoromethane
20109 citationsauthor #8
A Novel Autotaxin Inhibitor Reduces Lysophosphatidic Acid Levels in Plasma and the Site of Inflammation
2010225 citationsauthor #2
An analysis of the diaminopyrimidine patent estates describing spleen tyrosine kinase inhibitors by Rigel and Portola
201017 citationsauthor #3
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
201033 citationsauthor #16
An orally active inhibitor bound at the active site of HPGDS
20100 citationsauthor #3
Structure based design of novel irreversible FAAH inhibitors.
200910 citationsauthor #9
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
200953 citationsauthor #4
CDK-2-Cyclin complex with indazole inhibitor 9 bound at its active site
20090 citationsauthor #11
Synthesis of tert-butyl 6-oxo-2-azaspiro[3.3]heptane-2-carboxylate.
200919 citationsauthor #5
CDK-2 with indazole inhibitor 17 bound at its active site
20090 citationsauthor #11
Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics.
20089 citationsauthor #3
Preparation of novel anthranilic acids as antibacterial agents. Extensive evaluation of alternative amide bioisosteres connecting the A- and the B-rings.
200714 citationsauthor #1
Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.
20079 citationsauthor #1
Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles.
200716 citationsauthor #10
Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.
200713 citationsauthor #1
Advances in the discovery of novel antibacterial agents during the year 2002.
200438 citationsauthor #2
Immobilization of a novel antibacterial agent on solid phase and subsequent isolation of EF-Tu.
20049 citationsauthor #12
(R)‐(−)‐2,2‐Diphenylcyclopentanol
20034 citationsauthor #4
Oxazinoquinolones for treating viral infections
20010 citationsauthor #2
3-Arylpiperidines as potentiators of existing antibacterial agents.
200148 citationsauthor #1
Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition.
200127 citationsauthor #1
Corrigendum to “Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition” [Bioorg. Med. Chem. Lett. 11 (2001) 1355]†
20013 citationsauthor #1
Enols as potent antibacterial agents.
20012 citationsauthor #1
Palladium Catalyzed Bispyrimidine Thioether Synthesis
199914 citationsauthor #3
Chiral Benzoquinones as a New Class of Ligands for Asymmetric Catalysis: Synthesis and Application to the Palladium(II)‐Catalyzed 1,4‐Dialkoxylation of 1,3‐Dienes.
19991 citationsauthor #3
Preparation of phospholipids highly enriched with n-3 polyunsaturated fatty acids by lipase
199988 citationsauthor #2
Palladium(II)-Catalyzed Asymmetric 1,4-Oxidation of 2-Phenyl-1,3-cyclohexadiene.
19980 citationsauthor #1
EFFICIENT SYNTHESIS OF SYMMETRICAL 2,5-DISUBSTITUTED BENZOQUINONES VIA PALLADIUM-CATALYZED DOUBLE NEGISHI COUPLING
199828 citationsauthor #2
CHIRAL BENZOQUINONES AS A NEW CLASS OF LIGANDS FOR ASYMMETRIC CATALYSIS : SYNTHESIS AND APPLICATION TO THE PALLADIUM(II)-CATALYZED 1,4-DIALKOXYLATION OF 1,3-DIENES
199836 citationsauthor #3
Efficient Synthesis of Symmetrical 2,5-Disubstituted Benzoquinones via Palladium-Catalyzed Double Negishi Coupling.
19983 citationsauthor #2
A Versatile Route to 2-Substituted Cyclic 1,3-Dienes via a Copper(I)-Catalyzed Cross-Coupling Reaction of Dienyl Triflates with Grignard Reagents.
199831 citationsauthor #3
A Versatile Route to 2-Substituted Cyclic 1,3-dienes via a Copper(I)-Catalyzed Cross-Coupling Reaction of Dienyl Triflates with Grignard Reagents.
19980 citationsauthor #3
Tandem (4 + 2)/(3 + 2) Cycloadditions of Nitroalkenes. Part 9. Synthesis of (‐)‐Rosmarinecine.
19970 citationsauthor #2
Palladium(II)-catalyzed asymmetric 1,4-oxidation of 2-phenyl-1,3-cyclohexadiene
199725 citationsauthor #1
Tandem (4 + 2)/(3 + 2) Cycloadditions of Nitroalkenes. Part 10. trans‐ 2‐(1‐Methyl‐1‐phenylethyl)cyclohexanol as a New Auxiliary.
19970 citationsauthor #2
Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 11. The Synthesis of (+)-Crotanecine
199754 citationsauthor #2
Erratum: Tandem [4 + 2]/[3 + 2] cycloadditions of nitroalkenes. 10. trans-2-(1-methyl-1-phenylethyl)cyclohexanol as a new auxiliary (Journal of Organic Chemistry (1996) 61 (6728))
19970 citationsauthor #2
Tandem [4+2]/[3+2] Cycloadditions of Nitroalkenes.
1996528 citationsauthor #2
Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 10. trans-2-(1-Methyl-1-phenylethyl)cyclohexanol as a New Auxiliary.
19965 citationsauthor #2
(2aS,3S,6S,7S,7bR)-7-[(dimethylphenyl)-silyl]-2-oxo-6-[(1R,2S)-2- phenylcyclo-hexyloxy]-2a,3,6,7,7a,7b-hexahydro-2H-1,4,5-trioxa-4a- azacyclopenta[cd]indene-3-carboxylic acid 1-methylethyl ester.
19961 citationsauthor #1
The total syntheses of (+)-crotanecine, ( - )-hastanecine and ( - )-rosmarinecine utilizing the tandem (4+2)/(3+2) cycloadditions of nitroalkenes
19960 citationsauthor #1
A General Strategy for the Synthesis of Cis-Substituted Pyrrolizidine Bases. The Synthesis of (-)-Rosmarinecine
199522 citationsauthor #2
The Tandem Cycloaddition Chemistry of Nitroalkenes. A Novel Synthesis of (-)-Hastanecine.
19951 citationsauthor #2
Nitroalkene Inter [4 + 2]/Intra [3 + 2] Tandem Cycloadditions. 7. Application of (R)-(-)-2,2-Diphenylcyclopentanol as the Chiral Auxiliary
199531 citationsauthor #4
The Tandem Cycloaddition Chemistry of Nitroalkenes.
19950 citationsauthor #3
A General Strategy for the Synthesis of cis-Substituted Pyrrolizidine Bases. The Synthesis of (-)-Rosmarinecine (XIII).
19950 citationsauthor #2
Nitroalkene Inter (4+2)/Intra (3+2) Tandem Cycloadditions. Part 7. Application of (R)‐(‐)‐2,2‐Diphenylcyclopentanol as the Chiral Auxiliary.
19950 citationsauthor #4
The Tandem Cycloaddition Chemistry of Nitroalkenes. A Novel Synthesis of (-)-Hastanecine
199438 citationsauthor #2
The tandem cycloaddition chemistry of nitroalkenes
19947 citationsauthor #3
The generation of glyceryl ether lipids highly enriched with eicosapentaenoic acid and docosahexaenoic acid by lipase
199421 citationsauthor #2

TIMELINE

1994 66 citations

1995 54 citations

1996 534 citations

1997 79 citations

1998 98 citations

1999 103 citations

2001 80 citations

2003 4 citations

2004 47 citations

2007 52 citations

2008 9 citations

2009 82 citations

2010 306 citations

2011 48 citations

2012 60 citations

2014 65 citations

2016 306 citations

2017 197 citations

2018 88 citations

2019 129 citations

2020 45 citations

2023 16 citations

2024 11 citations

2025 9 citations

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