M. Covington

发表

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.

H. Kantarjian, T. Manshouri, A. Quintás-Cardama, 2010, Blood.

Discovery of γ-Lactam Hydroxamic Acids as Selective Inhibitors of Tumor Necrosis Factor α Converting Enzyme: Design, Synthesis, and Structure−Activity Relationships

Chen Lihua, Zelda R. Wasserman, Karl D. Hardman, 2002 .

Pharmacokinetics and Pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-Amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a Potent and Selective Inhibitor of Tumor Necrosis Factor α-Converting Enzyme in Rodents, Dogs, Chimpanzees, and Humans

J. Trzăskos, T. Maduskuie, C. Garner, 2007, Drug Metabolism and Disposition.

Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors

R. Copeland, R. Magolda, J. Trzăskos, 1996 .

Synthesis and structure–activity relationship of a novel, non-hydroxamate series of TNF-α converting enzyme inhibitors

A. Tebben, B. W. King, M. Covington, 2007 .

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.

M. Covington, C. Decicco, J. Duan, 2005, Bioorganic & medicinal chemistry letters.

Identification and Characterization of INCB 9471 , an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011 .

Identification and Characterization of INCB9471, an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011, Journal of Pharmacology and Experimental Therapeutics.

Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy

H. Koblish, M. Stubbs, Q. Wang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.

R. Magolda, M. Covington, C. Decicco, 2001, Journal of medicinal chemistry.

Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

M. Covington, C. Decicco, R. Wexler, 2002, Bioorganic & medicinal chemistry letters.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies

R. Wynn, A. Margulis, H. Koblish, 2018, PloS one.

Macrocyclic amino carboxylates as selective MMP-8 inhibitors.

W. DeGrado, K. D. Hardman, R. Copeland, 1998, Journal of medicinal chemistry.

Developing a JAK Inhibitor for Targeted Local Delivery: Ruxolitinib Cream

M. Covington, S. Shepard, S. Yeleswaram, 2021, Pharmaceutics.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

P. Scherle, K. Vaddi, M. Covington, 2011, ACS medicinal chemistry letters.

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

G. Trainor, M. Covington, C. Decicco, 2005, Journal of medicinal chemistry.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.

I. Kariv, K. Vaddi, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

High-level expression in Escherichia coli of a soluble and fully active recombinant interleukin-1 beta.

Y. Lin, M. Covington, R. Newton, 1987, Molecular biology & medicine.

Selective Inhibition of Eosinophil Influx into the Lung by Small Molecule CC Chemokine Receptor 3 Antagonists in Mouse Models of Allergic Inflammation

K. McIntyre, S. Mandlekar, J. Trzăskos, 2006, Journal of Pharmacology and Experimental Therapeutics.

A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity

R. Wynn, H. Koblish, X. Wen, 2020, Frontiers in Oncology.

Abstract 3759: Characterization of INCB081776, a potent and selective dual AXL/MER kinase inhibitor

R. Wynn, X. Liu, H. Koblish, 2018, Immunology.

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

J. Fridman, Jun Li, X. Wen, 2010, The Journal of Immunology.

Selective Inhibition of JAK 1 and JAK 2 Is Efficacious in Rodent Models of Arthritis : Preclinical Characterization of INCB 028050

J. Fridman, Jun Li, X. Wen, 2010 .

Preclinical Characterization of INCB 028050 Efficacious in Rodent Models of Arthritis : Selective Inhibition of JAK 1 and JAK 2 Is

J. Fridman, Jun Li, X. Wen, 2010 .

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.

G. Trainor, M. Covington, C. Decicco, 2002, Bioorganic & medicinal chemistry letters.

INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions.

P. Scherle, L. Leffet, Yanlong Li, 2012, European journal of pharmacology.

Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Jun Yu Li, M. Favata, P. Scherle, 2020, European journal of pharmacology.

Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-α production

K. D. Hardman, R. Copeland, B. Jaffee, 1999 .

COMPARISON OF SNAKE VENOM REPROLYSIN AND MATRIX METALLOPROTEINASES AS MODELS OF TNF-α CONVERTING ENZYME

J. Fox, G. Davis, R. Copeland, 1997 .

Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

J. Trzăskos, W. Marshall, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.

D. J. Nelson, K. D. Hardman, R. Copeland, 2001, Journal of medicinal chemistry.

Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors.

Yvonne Lo, M. Covington, S. Diamond, 2022, ACS medicinal chemistry letters.

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

H. Koblish, P. Scherle, T. Maduskuie, 2019, ACS medicinal chemistry letters.

Discovery of a novel 2-spiro-proline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

R. Wynn, P. Scherle, Yanlong Li, 2022, Bioorganic & medicinal chemistry letters.

Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Comparative effects of selective cyclooxygenase 1 and cyclooxygenase 2 inhibitors on myeloperoxidase and 3 alpha-hydroxysteroid dehydrogenase.

R. Copeland, J. Williams, J. Trzăskos, 1996, Journal of enzyme inhibition.

The Total Chemical Synthesis of Monocyte Chemotactic Protein‐1 (MCP‐1)

M. Covington, R. Newton, Angus R. Brown, 1996, Journal of peptide science : an official publication of the European Peptide Society.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, L. Leffet, 2005, The Journal of Immunology.

Amide surrogates of matrix metalloproteinase inhibitors : Urea and sulfonamide mimics

D. J. Nelson, R. Magolda, M. Covington, 1997 .

2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.

G. Trainor, M. Covington, C. Decicco, 2006, Bioorganic & medicinal chemistry letters.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.

D. J. Rogier, Wei Huang, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

2'-substituted chalcone derivatives as inhibitors of interleukin-1 biosynthesis.

D. G. Jones, M. Covington, R. Newton, 1993, Journal of medicinal chemistry.

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Soong-Hoon Kim, W. Pitts, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)

David D. Christ, K. Vaddi, M. Covington, 2008 .

Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.

Zelda R Wasserman, J. Trzăskos, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.

J. Trzăskos, K. Vaddi, M. Covington, 2008, Bioorganic & medicinal chemistry letters.

Conversion of potent MMP inhibitors into selective TACE inhibitors.

Bryan W King, B. W. King, M. Covington, 2006, Bioorganic & medicinal chemistry letters.

Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase.

R. Copeland, J. Williams, J. Trzăskos, 1994, Proceedings of the National Academy of Sciences of the United States of America.

Design, Synthesis, and Evaluation of Benzothiadiazepine Hydroxamates as Selective Tumor Necrosis Factor-α Converting Enzyme Inhibitors

S. Mandlekar, K. D. Hardman, R. Magolda, 2003 .

Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.

R. Copeland, J. Trzăskos, M. Covington, 1995, Journal of medicinal chemistry.

Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.

Xiaohua He, John Roderick, J. Trzăskos, 2004, Bioorganic & medicinal chemistry letters.

Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.

J. Trzăskos, K. Vaddi, M. Covington, 2008, Bioorganic & medicinal chemistry letters.

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

John Roderick, Xiao-tao Chen, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.

B. Jaffee, R. Magolda, J. Trzăskos, 2001, Journal of Medicinal Chemistry.

A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.

J. Trzăskos, Xiao-tao Chen, K. Vaddi, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and structure–activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors

J. Trzăskos, T. Maduskuie, B. W. King, 2004 .

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.

Xiaohua He, John Roderick, R. Magolda, 2003, Bioorganic & medicinal chemistry letters.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

A biochemical and kinetic analysis of the interleukin-1 receptor. Evidence for differences in molecular properties of IL-1 receptors.

R. Horuk, M. Covington, R. Newton, 1987, The Journal of biological chemistry.

Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

P. Scherle, Yanlong Li, M. Covington, 2009, Bioorganic & medicinal chemistry letters.

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

S. Mandlekar, K. D. Hardman, R. Magolda, 2003, Journal of medicinal chemistry.

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

D. J. Rogier, P. Scherle, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2002, Journal of medicinal chemistry.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Lixin Shao, Michael Xia, D. J. Rogier, 2011, ACS medicinal chemistry letters.

Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.

R. Wynn, P. Scherle, F. Baribaud, 2009, Biochemical and biophysical research communications.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, T. Burn, 2005, The Journal of Immunology.

Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

M. Covington, S. Diamond, S. Yeleswaram, 2022, ACS medicinal chemistry letters.

Muteins of human interleukin‐1 that show enhanced bioactivities

R. Horuk, J. B. Matthew, M. Covington, 1987, FEBS letters.

Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells

R. Wynn, P. Scherle, Phillip C. C. Liu, 2006, Cancer biology & therapy.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

R. Wynn, H. Koblish, Yue Zhang, 2020, PloS one.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies

Jun Yu Li, R. Wynn, X. Liu, 2018, Clinical Cancer Research.

Renal abnormalities and an altered inflammatory response in mice lacking cyclooxygenase II

J. Johnston, B. Jaffee, B. Car, 1995, Nature.

The distribution and clearance of radiolabeled human interleukin-1 beta in mice.

M. Covington, R. Newton, J. Uhl, 1988, Lymphokine research.

Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes.

M. Favata, A. J. Daulerio, R. Magolda, 1998, Journal of immunology.

Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL

H. Koblish, P. Scherle, T. Maduskuie, 2015 .

Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies

R. Wynn, X. Liu, X. Wen, 2017 .

Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab

J. Fridman, P. Scherle, K. Vaddi, 2006, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

R. Wynn, J. Fridman, P. Scherle, 2009, Bioorganic & Medicinal Chemistry Letters.

Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

K. D. Hardman, J. Trzăskos, M. Covington, 2004, Journal of medicinal chemistry.

Lipopolysaccharide-Stimulated Monocytes Production in 2 Cytokine and Prostaglandin E Inhibition of MAP Kinase Kinase Prevents

M. Favata, A. J. Daulerio, R. Magolda, 1998 .

Biology of TACE inhibition

K. Vaddi, M. Covington, P. Haley, 2001, Annals of the rheumatic diseases.

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.

H. Koblish, M. Deller, R. Klabe, 2022, Journal of medicinal chemistry.

The activation of human fibroblast prostaglandin E production by interleukin 1.

M. Covington, R. Newton, 1987, Cellular immunology.

Design, Synthesis, and Structure−Activity Relationships of Macrocyclic Hydroxamic Acids That Inhibit Tumor Necrosis Factor α Release in Vitro and in Vivo

Chen Lihua, Robert A. Copeland, David J. Nelson, 2001 .

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

R. Wynn, H. Koblish, Yue Zhang, 2021, Journal of medicinal chemistry.

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.

R. Magolda, J. Trzăskos, K. Vaddi, 2004, Bioorganic & medicinal chemistry letters.

Abstract 4904: The BET inhibitor INCB054329 enhances the activity of checkpoint modulation in syngeneic tumor models

H. Koblish, Yue Zhang, M. Stubbs, 2016 .

Inhibition of cytokine signaling by ruxolitinib and implications for COVID-19 treatment

T. Burn, Yanlong Li, M. Covington, 2020, Clinical Immunology.

Abstract 3780: Activity of the BET inhibitor INCB054329 in models of lymphoma

M. Stubbs, M. Favata, P. Scherle, 2016 .

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

M. Bower, R. Wynn, J. Fridman, 2007, Journal of medicinal chemistry.

Abstract 4712: Discovery of INCB059872, a novel FAD-directed LSD1 inhibitor that is effective in preclinical models of human and murine AML

R. Wynn, A. Margulis, X. Liu, 2016 .

Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.

R. Copeland, R. Magolda, J. Trzăskos, 1999, Bioorganic & medicinal chemistry letters.

Abstract 3523: Discovery of a novel BET inhibitor INCB054329

R. Wynn, X. Liu, Jun Li, 2015 .

Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.

April Horsey, L. Leffet, M. Covington, 2023, ACS Medicinal Chemistry Letters.

The fate of pro-TNF-alpha following inhibition of metalloprotease-dependent processing to soluble TNF-alpha in human monocytes.

M. Covington, C. Decicco, R. Newton, 1997, Journal of immunology.

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3

H. Koblish, M. Deller, R. Klabe, 2022, Journal of Medicinal Chemistry.

Abstract 2648: L-arginine regulates chemotherapy sensitivity via ER stress and autophagic pathways in arginine prototrophic cancer cells

H. Koblish, T. Burn, M. Covington, 2020 .

Characterization of murine IL-1 beta. Isolation, expression, and purification.

Y. Lin, R. Horuk, M. Covington, 1988, Journal of immunology.

Characterization of a Novel Rodent-Active Discovery and Pharmacological

P. Scherle, F. Baribaud, L. Leffet, 2013 .

Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.

D. J. Rogier, A. Bahinski, P. Scherle, 2011, Bioorganic & medicinal chemistry letters.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab.

J. Fridman, P. Scherle, K. Vaddi, 2006, Cancer Biology & Therapy.

Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor

R. Wynn, Yue Zhang, H. Koblish, 2022, Cancer discovery.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.