The average timeline from validated hit to preclinical candidate delivery in drug discovery is approximately four years. To shorten this timespan, Direct‑to‑Biology strategies are increasingly employed to accelerate early decision‑making and advance compound progression.

Our approach, Direct‑to‑Discovery, extends this even further, integrating not just chemistry and biology, but also DMPK and structural biology earlier into the process.

Harnessing the expertise of our high-throughput chemistry team, we reliably identify and validate assay compliant conditions across diverse reaction types. Coupled with our deep understanding of assay endpoints for CRMs, we deliver data that accelerates early decision making and drives compound progression.

Standard D2B workflows often focus primarily on affinity or efficacy measurements from CRMs, overlooking the broader value of this rich data source. To unlock this potential, we have expanded the approach through integrated methods, including Direct-to-Crystallography (D2C) and Direct–to-Physiochemistry and DMPK (D2DMPK), providing molecular level binding insight and detailed SAR directly from CRMs.

Feeding all this information into machine learning models completes the DMTA cycle and supports the use of AI to design future modifications.

Laboratory setting showing scientists working with glassware and reagents, representing medicinal chemistry for optimizing drug profiles and advancing compounds toward clinical development.

Direct-to-Biology Expertise

At Sygnature, we take a connected approach to compound optimisation, breaking down disciplinary silos to deliver better outcomes for our customers. This collaboration is essential for Direct‑to‑Biology, where understanding the composition of a CRM, and how it influences assay readouts, is critical for selecting the most appropriate chemistry and target dependant endpoint.

A forensic, connected mindset

Applying the strategy at the right time

Libraries designed for decision‑making

Key Strengths

Assay-Ready Chemistry

Automated High-Throughput Synthesis

Flexible bioassay integration

Real Time Structural Insights

Fast Metabolic Stability Readouts

Fully Integrated Degrader Discovery

Typical Applications

Fragment-based Drug Discovery – Integrating D2B and D2C to accelerate the identification of novel protein binders.

Early hit expansion – A data‑intensive phase of drug discovery where the rapid generation of SAR using D2B can be exceptionally powerful.

Rapid SAR generation during Hit to Lead or Lead Optimization – Enables fast, efficient use of resources and accelerates optimisation at any stage of the programme.

Targeted protein degradation – Provides the throughput needed to uncover new molecular glues and PROTACs, which are challenging to design using traditional methods.

Why Choose Sygnature Discovery for Direct to Biology Support?

Our Direct-to-Discovery platform isn’t just about going faster; it’s about changing the cadence of discovery. When chemical synthesis, biological testing, structural information and DMPK profiling run essentially in parallel:

  • Hit expansion accelerates – chemistry output can be triaged immediately, prioritizing the most promising analogues for full synthesis and purification
  • Decision points come earlier – unproductive chemical space is abandoned sooner, conserving resources
  • Biology drives chemistry – assay results feed directly back into design, guiding the next synthetic steps with live data

The result: weeks compressed into days, and SAR intelligence generated in near real-time.

Loading…
Integrating Hit Finding and Direct-to-Biology to Shorten Time to Development Candidate
Integrating Hit Finding and Direct-to-Biology to Shorten Time to Development Candidate
Helicases have been implicated in the progression of microsatellite instability-high (MSI-H) tumours and therefore represent…
Posters

Related Solutions

Chemistry
Hit Identification
Lead Optimization
High Throughput Chemistry
Bioscientist
DMPK
Targeted Protein Degradation
Protein & Structure