ArticleMolecular pharmacology2018
Small-Molecule Positive Allosteric Modulators of the
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In one paragraph
Article in Molecular pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
0numbers the graph read from it
0cells of the map it votes in
46citing papers in PubMed
3.3field-weighted citation impact, top 7% of its field
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
46 citing papers in PubMed, 90 citations in OpenAlex.
- Agonist-specific conformational dynamics at the βBritish journal of pharmacology · 2026Article
- Discovery of membrane channel modulators via DNA encoded library screening using native like membrane protein nanoparticles.Scientific reports · 2026Article
- Recent Advances in GPCR Ligand Discovery Using DNA-Encoded Library Technology: From Affinity Binding to Functional Bias and Allosteric Modulation.ACS medicinal chemistry letters · 2026Review
- Discovery and dynamic pharmacology of μ-opioid receptor positive allosteric modulators.bioRxiv : the preprint server for biology · 2026Article
- Biased Allosteric Modulation in GPCR Drug Discovery.Handbook of experimental pharmacology · 2026Review
- Biased Orthosteric Agonism and Allosteric Modulation: Emerging Strategies for Developing New Class of β-Agonists for Obstructive Airway Diseases.American journal of respiratory cell and molecular biology · 2025Review
- Gut-heart axis: cardiac remodeling and heart failure in the context of inflammatory bowel disease and dysbiosis.American journal of physiology. Gastrointestinal and liver physiology · 2025Review
- Implication of Central βArchiv der Pharmazie · 2025Review
- Structure and dynamics determine G protein coupling specificity at a class A GPCR.Science advances · 2025Article
- A non-canonical mechanism of GPCR activation.Nature communications · 2024Article
- Gut microbe-generated phenylacetylglutamine is an endogenous allosteric modulator of β2-adrenergic receptors.Nature communications · 2024Article
- A data science roadmap for open science organizations engaged in early-stage drug discovery.Nature communications · 2024Review
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- The M3 Muscarinic Acetylcholine Receptor Can Signal through Multiple G Protein Families.Molecular pharmacology · 2024Article
- β-adrenergic receptor signaling mediated by β-arrestins and its potential role in heart failure.Current opinion in physiology · 2024Article
- Inhibitors of Immune Checkpoints: Small Molecule- and Peptide-Based Approaches.Journal of personalized medicine · 2024Review
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Allosteric modulator potentiates β2AR agonist-promoted bronchoprotection in asthma models.The Journal of clinical investigation · 2023Article
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Identification of a β-arrestin-biased negative allosteric modulator for the βProceedings of the National Academy of Sciences of the United States of America · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
19 authors at 4 institutions in 2 countries.
Seungkirl AhnDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Biswaranjan PaniDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Alem W KahsaiDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Eva K OlsenDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Gitte HusemoenDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Mikkel VestergaardDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Lei JinDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Shuai ZhaoDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Laura M WinglerDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Paula K RambaratDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Rishabh K SimhalDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Thomas T XuDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Lillian D SunDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Paul J ShimDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Dean P StausDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Li-Yin HuangDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Thomas FranchDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Xin ChenDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.).
Robert J LefkowitzDepartments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.) lefko001@receptor-biol.duke.edu.
Changzhou University · CNDuke Medical Center · USDuke University · USHoward Hughes Medical Institute · US
Funding
Molecular Regulation of Cardiovascular 7 TM ReceptorsR01HL016037 · NHLBI · DUKE UNIVERSITY · PI ROBERT J LEFKOWITZ · 1985 to 2026
$14.5MMULTIDISCIPLINARY HEART &VASCULAR DISEASEST32HL007101 · NHLBI · DUKE UNIVERSITY · PI FREEDMAN, NEIL J. · 1985 to 2020
$9.8MHoward Hughes Medical InstituteNHLBI NIH HHS R01 HL016037NHLBI NIH HHS T32 HL007101
Abstract
Conventional drug discovery efforts at the
Indexed as
Adrenergic beta-2 Receptor AgonistsAllosteric RegulationAllosteric Sitebeta-Arrestin 1Drug SynergismGene LibraryGTP-Binding ProteinsMolecular StructureReceptors, Adrenergic, beta-2Small Molecule LibrariesStructure-Activity RelationshipSubstrate SpecificityAdrenergic beta-2 Receptor Agonistsbeta-Arrestin 1GTP-Binding ProteinsReceptors, Adrenergic, beta-2Small Molecule Libraries
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