Structure‐based discovery of ( S )‐2‐amino‐6‐(4‐fluorobenzyl)‐5,6,11,11a‐tetrahydro‐1H‐imidazo[1',5':1,6]pyrido[3,4‐b]indole‐1,3(2H)‐dione as low nanomolar, orally bioavailable autotaxin inhibitor

Macrophage Depletion Reveals an Active Role of the Immune System in Determining the In Vivo Disposition of an Orally Bioavailable Drug

10.26226/morressier.57d6b2bbd462b8028d88eb6e ◽

2016 ◽

Author(s):

Phillip Rzeczycki

Keyword(s):

Immune System ◽

Active Role ◽

Macrophage Depletion ◽

Orally Bioavailable

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Faculty Opinions recommendation of Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1046522.496495 ◽

2006 ◽

Author(s):

Andrew Combs

Keyword(s):

Hepatitis C Virus ◽

Hepatitis C ◽

Protease Inhibitor ◽

Therapeutic Agent ◽

Hepatitis C Infection ◽

Potential Therapeutic Agent ◽

Orally Bioavailable ◽

Ns3 Protease

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Faculty Opinions recommendation of Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1080870.533803 ◽

2007 ◽

Author(s):

Thomas W von Geldern

Keyword(s):

Receptor Antagonists ◽

B1 Receptor ◽

Bradykinin B1 Receptor ◽

Orally Bioavailable

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Faculty Opinions recommendation of Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.13357116.14726431 ◽

2011 ◽

Author(s):

Manoj Desai ◽

Dmitry Koltun

Keyword(s):

Kinase Inhibitor ◽

Pi3 Kinase ◽

Class I ◽

Orally Bioavailable

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Faculty Opinions recommendation of Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.14208965.15726072 ◽

2012 ◽

Author(s):

David Rotella

Keyword(s):

Orally Bioavailable

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Faculty Opinions recommendation of Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.718319734.793492567 ◽

2014 ◽

Author(s):

Jefferson Tilley

Keyword(s):

Inverse Agonist ◽

Ghrelin Receptor ◽

Orally Bioavailable ◽

Receptor Inverse Agonist ◽

Clinical Candidate

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Faculty Opinions recommendation of Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.718490794.793514568 ◽

2016 ◽

Author(s):

Wade Blair

Keyword(s):

Orally Bioavailable

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Faculty Opinions recommendation of Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.718490794.793497461 ◽

2014 ◽

Author(s):

John Lowe

Keyword(s):

Orally Bioavailable

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Faculty Opinions recommendation of Treatment with an orally bioavailable prodrug of 17β-estradiol alleviates hot flushes without hormonal effects in the periphery.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.726596256.793523523 ◽

2016 ◽

Author(s):

Darrell Brann

Keyword(s):

Hot Flushes ◽

Hormonal Effects ◽

17Β Estradiol ◽

Orally Bioavailable

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X-ray Structure-Guided Discovery of a Potent, Orally Bioavailable, Dual Human Indoleamine/Tryptophan 2,3-Dioxygenase (hIDO/hTDO) Inhibitor That Shows Activity in a Mouse Model of Parkinson’s Disease

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c00303 ◽

2021 ◽

Author(s):

Xiang-Li Ning ◽

Yu-Zhi Li ◽

Cui Huo ◽

Ji Deng ◽

Cheng Gao ◽

...

Keyword(s):

Parkinson’S Disease ◽

Parkinson's Disease ◽

Mouse Model ◽

Guided Discovery ◽

X Ray ◽

Orally Bioavailable

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