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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

Journal of medicinal chemistry, 2017-03, Vol.60 (5), p.1971-1993

2017

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Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10665-10699

2018

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Implementation of combined approaches to quantify plasma protein binding of bRo5 compounds

Drug metabolism and pharmacokinetics, 2024-04, Vol.55, p.100912, Article 100912

2024

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Target the More Druggable Protein States in a Highly Dynamic Protein–Protein Interaction System

Journal of chemical information and modeling, 2016-01, Vol.56 (1), p.35-45

2016

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Structural basis for CCR6 modulation by allosteric antagonists

Nature communications, 2024-08, Vol.15 (1), p.7574-13, Article 7574

2024

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A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation

The Journal of pharmacology and experimental therapeutics, 2010-07, Vol.334 (1), p.310-317

2010

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Meet Our Associate Editor

Recent patents on anti-infective drug discovery, 2020-12, Vol.15 (2), p.87-88

Thorarensen, Atli

2020

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Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (11), p.3795-3799

2012

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Advances in the discovery of novel antibacterial agents during the year 2002

Current medicinal chemistry, 2004-08, Vol.11 (16), p.2213-2243

2004

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Meet Our Associate Editor

Recent patents on anti-infective drug discovery, 2015-11, Vol.10 (2), p.70-70

Thorarensen, Atli

2015

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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

Bioorganic & medicinal chemistry, 2021-01, Vol.29, p.115865-115865, Article 115865

2021

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Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 11. The Synthesis of (+)-Crotanecine

Journal of the American Chemical Society, 1997-01, Vol.119 (1), p.125-137

1997

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PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor

ACS chemical biology, 2019-06, Vol.14 (6), p.1235-1242

2019

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From in silico to in Vitro to In Vivo : Increasing Megakaryocytes to Treat Thrombocytopenia

Blood, 2023-11, Vol.142 (Supplement 1), p.5580-5580

2023

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Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor

Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (16), p.4646-4649

2007

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New spleen tyrosine kinase inhibitors: patent applications published during 2011-2013

Pharmaceutical patent analyst, 2014-09, Vol.3 (5), p.523-541

2014

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Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms

Drug metabolism and disposition, 2017-01, Vol.45 (1), p.1-7

2017

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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

The Journal of pharmacology and experimental therapeutics, 2023-07, Vol.386 (1), p.80-92

2023

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Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 9. Synthesis of (−)-Rosmarinecine

Journal of the American Chemical Society, 1996-09, Vol.118 (35), p.8266-8277

1996

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ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

ACS chemical biology, 2014-07, Vol.9 (7), p.1552-1558

2014

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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

Journal of organic chemistry, 1998-09, Vol.63 (19), p.6466-6471

1998

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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

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10415-10439

2018

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Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide

Scientific reports, 2016-05, Vol.6 (1), p.26071, Article 26071

2016

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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

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Implementation of combined approaches to quantify plasma protein binding of bRo5 compounds

Target the More Druggable Protein States in a Highly Dynamic Protein–Protein Interaction System

Structural basis for CCR6 modulation by allosteric antagonists

A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation

Meet Our Associate Editor

Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters

Advances in the discovery of novel antibacterial agents during the year 2002

Meet Our Associate Editor

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

Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 11. The Synthesis of (+)-Crotanecine

PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor

From in silico to in Vitro to In Vivo : Increasing Megakaryocytes to Treat Thrombocytopenia

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

New spleen tyrosine kinase inhibitors: patent applications published during 2011-2013

Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)

Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms

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

Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 9. Synthesis of (−)-Rosmarinecine

ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

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

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

Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide

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