The workspace for preclinical decisions

How it works
01 / 04
Evaluate activity, selectivity, DMPK and safety against programme criteria, with measured and predicted results clearly distinguished.

Every conclusion, open to review
Trace conclusions to their sources, experimental conditions and model versions. Review applicability and uncertainty, with observations, predictions and mechanistic hypotheses kept separate.
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- Programme
- Covalent KRAS G12C series, 214 analogues
- Decision examined
- Which analogue carries the exposure margin to a toxicology study
- Measurements available
- Covalent kinetics, HLM stability, free fraction, permeability, hERG, CYP3A4 TDI
- Limiting finding
- Margin capped by CYP3A4 oxidation at the position being used as a potency handle
- Recommendation
- Advance OPS-SM-118, at 11x unbound margin and 12 percent lower covalent potency
- Validation status
- Confirmed by metabolite identification; rat margin remains at 1.7x and open
Bring one programme into Octopus
We start from the data you already hold, and show what it supports before anything new is run.
Discuss your programme