Drug Modalities

LMw & Biologics

Excellerate applies tailored strategies to optimize the efficacy and safety of small molecules and biologics, ensuring a comprehensive understanding of their pharmacological properties.

Our expertise supports characterization of drug interactions, signaling dynamics, and off-target effects to inform your decision-making in lead optimization.

• Target Interactions & Signaling Modulation: LMw compounds regulation of intracellular pathways (reversible vs covalent modification), biologics effects on e.g. extracellular receptors or cytokine signaling.
• Efficacy Determination: Small molecule IC₅₀/EC₅₀ and kinetic binding analysis, biologics affinity, avidity, and neutralization potency.
• Selectivity & Bias Analysis: E.g. pathway bias assessment, selective engagement optimization (e.g. Fc modifications, bispecific designs).
• Cytotoxicity & Off-Target Effects: Small molecules dose-dependent cytotoxicity panel screening, biologics immunogenicity risk evaluation.
• Phenotypic Assays for Safety Profiling: Cellular stress, apoptosis, and immune response evaluation for early toxicity assessment.

Orthosteric & Allosteric Interactions

Excellerate provides comprehensive analysis of drug-target interactions and mechanism of action, supporting the characterization of both orthosteric and allosteric modulators.

• Binding Assays: Bespoke development of equilibrium and kinetic binding assays e.g. TR-FRET and NanoBRET platforms.

• Saturation & Competition Binding: Assessment of ligand affinity, receptor occupancy, and competitive interactions.

• Kinetic Binding Analysis: Measurement of association/dissociation rates to determine target engagement and residence time.

• Signaling Kinetics: Quantification of ligand-induced signaling dynamics, including temporal pathway activation.

• Allosteric Modulation: Characterization of allosteric binding and functional effects, including modulation of orthosteric ligand activity.

• MOA Studies: Schild and Gaddum analysis to define competitive, non-competitive, and allosteric interaction profiles.

Kinetics & Covalent Inhibitors

Excellerate specializes in kinetic profiling to characterize drug-target interactions, binding dynamics and duration of action.

Our expertise extends to covalent inhibitors and complex mechanistic studies to support lead optimization.

• Competitive Kinetic Binding: Motulsky-Mahan analysis for detailed kinetic characterization of reversible inhibitors.

• MOA Enzymatic Studies: Quantification of enzyme kinetics e.g. substrate turnover and inhibitor potency.

• Covalent Inhibitor Profiling: Analysis of time-dependent target engagement, residence time, and kinetic selectivity.

• Complex MOA Analysis: Investigation of multi-step binding, conformational changes, and irreversible inhibition kinetics.

Innovative Biologics

Excellerate provides advanced assay platforms to characterize binding, function, and/or immunological activity of bispecific antibodies, ADCs, and ligand-directed therapies.

• Bispecific Binding Analysis: Quantification of dual-target engagement, affinity, and avidity using e.g. TR-FRET, NanoBRET, HTRF.

• Phenotypic Assays: Functional assessment of biologic-induced cellular responses, including proliferation, cytotoxicity, and differentiation.

• T-Cell Activation: Measurement of T-cell engagement, cytokine release, and immune activation in BiTE and checkpoint modulator studies.

• Antibody-Drug Conjugates (ADCs): Evaluation of payload delivery, internalization kinetics, and cytotoxic effects on target cells.

• Immunological Assays: Characterization of Fc receptor interactions, ADCC, and complement activation for immune-modulating biologics.

• Fluorescent Drug Localization: High-content imaging to track intracellular trafficking, receptor internalization, and subcellular distribution.

Next-Generation Therapies

Excellerate provides advanced assay solutions to evaluate next-generation therapies, including PROTACs, molecular glues, and innovative drug delivery systems.

Our platforms enable precise characterization of target modulation and therapeutic efficacy, supporting the development of novel treatments with improved specificity and potency.

• Ligase Engagement – High-sensitivity assays to quantify PROTAC and molecular glue-mediated E3 ligase recruitment and target degradation e.g. via NanoBRET or immunofluorescent approaches.

• Ligand-Induced Dimerization Assays – Customizable assays to assess ligand-induced target dimerization, enabling detailed mechanistic insights into drug action and PPI.

• Therapeutic Efficacy – Evaluation of cellular responses to drug candidates, including pathway modulation and functional outcomes.

Advanced Therapeutic Approaches

Excellerate offers cutting-edge assays to evaluate the efficacy of prodrugs, immunomodulators, and synergistic drug combinations.

Our platforms provide insights into drug activation, immune modulation, and combinational therapy outcomes, supporting the development of highly effective and targeted treatments.

• Phenotypic Assays – Functional assays to assess cellular responses to prodrugs and immunomodulators, including changes in proliferation, cytotoxicity, and differentiation.

• Primary Human Immune Cell Assays – In-depth analysis of immune cell activity and cytokine release in response to therapeutic agents, including T-cell, NK cell, and macrophage responses.

• Synergistic Combinations – Evaluation of drug-drug interactions, synergy, and combinatory effects in immune modulation and tumor response.

• Immunomodulation – Characterization of immune system modulation, including checkpoint inhibition, immune activation, and suppression pathways.