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Macrocycle Library
Macrocycle Library

Enrich your screening decks with enabled bRo5 starting points

Macrocycles are privileged structures in Medicinal Chemistry as they successfully expand the available Compound Space and have special features that make them druggable despite being beyond the Rule of 5 (bRo5).

About Macrocycles

Macrocycles are privileged structures in Medicinal Chemistry as they:

  • provide diverse functionality and stereochemical complexity in a conformationally pre-organized ring structure
  • are semi-rigid compounds, a compromise between structural pre-organization (entropy) and sufficient flexibility to mould to a target surface and maximize binding (induced fit)
  • can demonstrate drug-like physicochemical and good PK properties such as solubility, lipophilicity, metabolic stability, cell (and BBB) permeability and bioavailability beyond the Rule of 5
Macrocycle Library

Well-balanced properties

The SpiroQUEST™ Library was developed over several years to maximize chemical and topological diversity. The macrocycles (12-30 atoms) incorporate naturally occurring and non-natural amino acids as well as 1600+ non-peptidic linkers to vary ring size/nature, add heteroatoms, pharmacophores, and introduce conformational constraints.

Macrocycle Library

Well-balanced properties

The SpiroQUEST™ Library was developed over several years to maximize chemical and topological diversity. The macrocycles (12-30 atoms) incorporate naturally occurring and non-natural amino acids as well as 1600+ non-peptidic linkers to vary ring size/nature, add heteroatoms, pharmacophores, and introduce conformational constraints.

Macrocycle Library

Well-balanced properties

The SpiroQUEST™ Library was developed over several years to maximize chemical and topological diversity. The macrocycles (12-30 atoms) incorporate naturally occurring and non-natural amino acids as well as 1600+ non-peptidic linkers to vary ring size/nature, add heteroatoms, pharmacophores, and introduce conformational constraints.

Macrocycle Library

Well-balanced properties

The SpiroQUEST™ Library was developed over several years to maximize chemical and topological diversity. The macrocycles (12-30 atoms) incorporate naturally occurring and non-natural amino acids as well as 1600+ non-peptidic linkers to vary ring size/nature, add heteroatoms, pharmacophores, and introduce conformational constraints.

Macrocycle Library

Let’s work together

The apparent complexity of the structures is decorrelated from their synthetic accessibility.
The chemical space surrounding the SpiroQUEST™ Library is fully enabled thanks to our proprietary platform: SpiroChem guarantees rapid turn-around time for hit validation and downstream optimization work.

Step 1: Purchase of SpiroQUEST™ Library

Format

Available as 10mM DMSO solution

Standard volumes: 2 or 5uL

Plate format: greiner 784201

Other plate format available on request

Timelines

ca 1-2 weeks (if replating needed)

Pricing model

Fixed price*

Screening

Performed by Client or Third Party screening center

Note: SpiroChem has screening partners and can arrange/coordinate screening efforts on behalf of Client.

Timelines

TBD with Client/Third Party

Workflow
  • Hit analysis by SpiroChem
  • Preparation of a validation library of 48-96 analogues around selected hits
  • Unblinding* of hits
  • Resynthesis of hits and supply
Timelines

ca 6-8 weeks

Pricing model

Fee for Service* based on # of analogs

Workflow
  • Hit-to-Lead and Lead Optimization
Timelines

ca 6 weeks per synthesis cycle

Pricing model

FTE-based contract

* Contact us for our General Terms and Sales Conditions

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