ArticlePharmacology research & perspectives2017
A three-parameter two-state model of receptor function that incorporates affinity, efficacy, and signal amplification.
Article in Pharmacology research & perspectives, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Programmable synthetic cytokine receptors polarize macrophages to user-defined functional states.bioRxiv : the preprint server for biology · 2026Article
- The ability of SABRE, a new quantitative receptor function model, to quantify receptor binding from even challenging concentration-effect data with a single unified fit.Frontiers in pharmacology · 2026Article
- 8-Oxo-7,8-dihydropurines as Building Blocks to Enhance the Selectivity of an RNA Aptamer for Aminoglycosides.ACS chemical biology · 2025Article
- The flexibility of SABRE, a new quantitative receptor function model, when fitting challenging concentration-effect data.Frontiers in pharmacology · 2025Article
- Cooperative Gating of a KJournal of the American Chemical Society · 2024Article
- Zafirlukast Is a Promising Scaffold for Selectively Inhibiting TNFR1 Signaling.ACS bio & med chem Au · 2023Article
- Quantitative receptor model for responses that are left- or right-shifted versus occupancy (are more or less concentration sensitive): the SABRE approach.Frontiers in pharmacology · 2023Article
- Quantification of receptor binding from response data obtained at different receptor levels: a simple individual sigmoid fitting and a unified SABRE approach.Scientific reports · 2022Article
- A single unified model for fitting simple to complex receptor response data.Scientific reports · 2020Article
- Functional anatomy of the full-length CXCR4-CXCL12 complex systematically dissected by quantitative model-guided mutagenesis.Science signaling · 2020Article
- An Advanced In Silico Modelling of the Interaction between FSCPX, an Irreversible AMolecules (Basel, Switzerland) · 2019Article
- A Receptor Model With Binding Affinity, Activation Efficacy, and Signal Amplification Parameters for Complex Fractional Response Versus Occupancy Data.Frontiers in pharmacology · 2019Article
- Design, Synthesis, and Evaluation of Novel Immunomodulatory Small Molecules Targeting the CD40⁻CD154 Costimulatory Protein-Protein Interaction.Molecules (Basel, Switzerland) · 2018Article
- An evaluation of the operational model when applied to quantify functional selectivity.British journal of pharmacology · 2018Article
- Toward Small-Molecule Inhibition of Protein-Protein Interactions: General Aspects and Recent Progress in Targeting Costimulatory and Coinhibitory (Immune Checkpoint) Interactions.Current topics in medicinal chemistry · 2018Review
- A three-parameter two-state model of receptor function that incorporates affinity, efficacy, and signal amplification.Pharmacology research & perspectives · 2017Article
Corrections and comments
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1 author.
Funding
Abstract
A generalized model of receptor function is proposed that relies on the essential assumptions of the minimal two-state receptor theory (i.e., ligand binding followed by receptor activation), but uses a different parametrization and allows nonlinear response (transduction) for possible signal amplification. For the most general case, three parameters are used:
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.