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Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists

European journal of medicinal chemistry, 2023-03, Vol.250, p.115174-115174, Article 115174

2023

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Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity

The international journal of neuropsychopharmacology, 2018-10, Vol.21 (10), p.962-977

2018

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Determinants of Neutral Antagonism and Inverse Agonism in the β 2 -Adrenergic Receptor

Journal of chemical information and modeling, 2024-03, Vol.64 (6), p.2045-2057

2024

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Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16829-16859

2022

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Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

Nature (London), 2020-03, Vol.579 (7800), p.609-614

2020

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Histamine H 3 receptor antagonists/inverse agonists: Where do they go?

Pharmacology & therapeutics (Oxford), 2019-08, Vol.200, p.69

2019

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Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Nature (London), 2016-03, Vol.531 (7594), p.335-340

2016

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Transformation of a Dopamine D 2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents

Journal of medicinal chemistry, 2023-05, Vol.66 (9), p.6274-6287

2023

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Cannabinoid Receptors: Where They are and What They do

Journal of neuroendocrinology, 2008-05, Vol.20 (s1), p.10-14

Mackie, K.

2008

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(Inverse) Agonists of Retinoic Acid-Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease

Annual review of pharmacology and toxicology, 2020-01, Vol.60, p.371

2020

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Late-stage oxidative C(sp 3 )-H methylation

Nature (London), 2020-04, Vol.580 (7805), p.621-627

2020

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Structure, function and pharmacology of human itch GPCRs

Nature (London), 2021-12, Vol.600 (7887), p.170-175

2021

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Current topics in angiotensin II type 1 receptor research: Focus on inverse agonism, receptor dimerization and biased agonism

Pharmacological research, 2017-09, Vol.123, p.40-50

2017

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Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants

Journal of the American Chemical Society, 2024-03, Vol.146 (10), p.6522-6529

2024

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Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance

Pharmacological reviews, 2023-05, Vol.75 (3), p.416-462

2023

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Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor

The Journal of pharmacology and experimental therapeutics, 2023-08, Vol.386 (2), p.117

2023

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The Endogenous Retinoic Acid Receptor Pathway Is Exploited by Mycobacterium tuberculosis during Infection, Both In Vitro and In Vivo

The Journal of immunology (1950), 2023-08, Vol.211 (4), p.601-611

2023

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Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance

Cell metabolism, 2012-08, Vol.16 (2), p.167-179

2012

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An Inverse Agonist GSK5182 Increases Protein Stability of the Orphan Nuclear Receptor ERRγ via Inhibition of Ubiquitination

International journal of molecular sciences, 2022-12, Vol.24 (1), p.96

2022

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Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists

Future medicinal chemistry, 2024-02, Vol.16 (3), p.197-204

2024

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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists

Bioorganic & medicinal chemistry, 2023-01, Vol.78, p.117130-117130, Article 117130

2023

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The 5-HT 2A/2C inverse agonist nelotanserin alleviates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset

The European journal of neuroscience, 2024-03, Vol.59 (6), p.1169-1176

2024

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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Nature (London), 2011-05, Vol.474 (7352), p.521-525

2011

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GPR3 and GPR6, novel molecular targets for cannabidiol

Biochemical and biophysical research communications, 2017-08, Vol.490 (1), p.17-21

2017

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In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A 2A Receptor Antagonist/Inverse Agonist

Molecular pharmacology, 2023-06, Vol.103 (6), p.311-324

2023

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Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists

Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity

Determinants of Neutral Antagonism and Inverse Agonism in the β 2 -Adrenergic Receptor

Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

Histamine H 3 receptor antagonists/inverse agonists: Where do they go?

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Transformation of a Dopamine D 2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents

Cannabinoid Receptors: Where They are and What They do

(Inverse) Agonists of Retinoic Acid-Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease

Late-stage oxidative C(sp 3 )-H methylation

Structure, function and pharmacology of human itch GPCRs

Current topics in angiotensin II type 1 receptor research: Focus on inverse agonism, receptor dimerization and biased agonism

Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants

Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance

Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor

The Endogenous Retinoic Acid Receptor Pathway Is Exploited by Mycobacterium tuberculosis during Infection, Both In Vitro and In Vivo

Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance

An Inverse Agonist GSK5182 Increases Protein Stability of the Orphan Nuclear Receptor ERRγ via Inhibition of Ubiquitination

Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists

Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists

The 5-HT 2A/2C inverse agonist nelotanserin alleviates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

GPR3 and GPR6, novel molecular targets for cannabidiol

In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A 2A Receptor Antagonist/Inverse Agonist

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