Our breakthrough systems biology platform combines pharmacology, biology and mathematics to accelerate the hit-to-lead process in GPCR drug discovery
How It Works
1. G Protein Coupled Receptors & Ligands
Our platform is applicable to all GPCR targets, indication or type of compound, e.g. biologics or small molecules, full/partial agonists, antagonists, orthosteric or allosteric ligands. We perform all our assays using unlabeled ligands, thereby excluding labeling artefacts.
We express your target GPCR in cell lines containing signaling biosensors. We use a small set of reference ligands to calibrate the signaling responses of your target GPCR.
Our platform is applicable to all GPCR targets, indication or type of compound, e.g. biologics or small molecules, full/partial agonists, antagonists, orthosteric or allosteric ligands. We perform all our assays using unlabeled ligands, thereby excluding labeling artefacts.
We express your target GPCR in cell lines containing signaling biosensors. We use a small set of reference ligands to calibrate the signaling responses of your target GPCR.
2. Time resolved cellular signaling assays
We perform time-resolved cellular signaling assays to obtain kinetic profiles of your test compounds. This approach captures cellular signaling cascades to a much higher extent than static end-point assays.
We perform time-resolved cellular signaling assays to obtain kinetic profiles of your test compounds. This approach captures cellular signaling cascades to a much higher extent than static end-point assays.
3. Proprietary systems biology models
We generate mathematical models using ordinary differential equations (ODEs) to describe the specific signaling pathways of your target GPCR. We then analyze the kinetic profiles of your test compounds using this unique systems biology model.
We generate mathematical models using ordinary differential equations (ODEs) to describe the specific signaling pathways of your target GPCR. We then analyze the kinetic profiles of your test compounds using this unique systems biology model.
4. Clustering compounds based on novel parameters
Our systems biology analysis provides you with a multitude of novel ligand parameters. We then cluster your test compounds based on this analysis. We can easily spot outliers (off-target effects) and help you to identify compounds with the most promising profiles for in vivo testing
Our systems biology analysis provides you with a multitude of novel ligand parameters. We then cluster your test compounds based on this analysis. We can easily spot outliers (off-target effects) and help you to identify compounds with the most promising profiles for in vivo testing
5. Better prediction of in vivo effects
We can therefore assist in correlating the new compound parameter profiles to in vivo data provided by you – thereby honing in on promising compounds in an early stage. This accelerates the hit-to-lead identification process.
The InterAx Edge
Full ligand range
No limitations on ligand types
No ligand labeling
Ensuring better predictions
Time-resolved assays
More accurately characterize in-cell
behaviour
behaviour
The InterAx Edge
Full ligand range
No limitations on ligand types
No ligand labeling
Ensuring better predictions
Time-resolved assays
More accurately characterize in-cell
behaviour
behaviour
Asthma Case Study
We exemplified the power of our platform by predicting asthma drug action using our proprietary beta2-adrenergic receptor ODE model.
Supporting Literature
G Protein-Coupled Receptor Signaling Networks from a Systems Perspective
Roth S, Kholodenko BN, Smit MJ, Bruggeman FJ (2015). Mol Pharmacol., 88(3): 604-16.
Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking
Roed SN, Nøhr AC, Wismann P, Iversen H, Bräuner-Osborne H, Knudsen SM, Waldhoer M (2015). J Biol Chem. 290(2):1233-43.
Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking
Roed SN, Nøhr AC, Wismann P, Iversen H, Bräuner-Osborne H, Knudsen SM, Waldhoer M (2015). J Biol Chem. 290(2):1233-43.
The project PICARD has received funding from the European Union’s Horizon 2020 research and innovation program under grant agreement No 880322
AI Integration
As one of the few winners of the EU Horizon 2020 funding, InterAx is integrating artificial intelligence into its proprietary systems biology platform. The EU project is called PICARD and is aimed at further accelerating lead identification and enabling de novo drug design.
