Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents

Zhonghui Lu, Gregory R. Ott, Rajan Anand, +8

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryBiochemistryMedicineNatural Sciences +9

Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach

Jonathan E. Wilson, Ravi Kurukulasuriya, Mikhail Reibarkh, +14

ACS Medicinal Chemistry Letters

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

Chu‐Biao Xue, Hao Feng, Ganfeng Cao, +31

ACS Medicinal Chemistry Letters

Chemotaxis ActivityMolecular PharmacologyPotent Human Ccr2BiochemistryFunctional Selectivity +11

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

Gregory R. Ott, Naoyuki Asakawa, Zhonghui Lu, +9

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceBiochemistryMedicineTnf-α Converting Enzyme +9

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

Chu‐Biao Xue, Anlai Wang, Qi Han, +29

ACS Medicinal Chemistry Letters

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

Chu‐Biao Xue, Anlai Wang, David Meloni, +25

Bioorganic & Medicinal Chemistry Letters

Translational PharmacologyFunctional SelectivityMedicineMurine Ccr2Immunology +5

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

Changsheng Zheng, Ganfeng Cao, Michael Xia, +25

Bioorganic & Medicinal Chemistry Letters

MedicineImmunologyPharmacological AgentCcr5 AntagonistPharmacotherapy +5

Cyp1 Inhibition Prevents Doxorubicin‐Induced Cardiomyopathy in a Zebrafish Heart‐Failure Model

Pui‐Ying Lam, Peter S. Kutchukian, Rajan Anand, +14

ChemBioChem

Heart FailureCardiovascular PharmacologyPathologyPharmacotherapyCardiovascular Toxicity +15

A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV-1 Infected Cells

Keith P. Moore, Adam G. Schwaid, Matthew Tudor, +36

ACS Chemical Biology

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity

Chu‐Biao Xue, Lihua Chen, Ganfeng Cao, +28

ACS Medicinal Chemistry Letters

Hiv-1 Entry InhibitorImmunologyMolecular BiologyCcr5 AntagonistPharmacotherapy +15