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Lead optimization is a key process in identifying preclinical candidates. The most promising hit series, once they are identified through hit-to-lead efforts, will advance into the lead optimization stage of drug discovery. The goal of this stage is to optimize, in parallel, both the biological activity and the properties of the lead series, through a dedicated screening funnel of both in vitro and in vivo assays. Screening assays are also designed to evaluate the physiochemical properties to determine the best compound to be formulated and dosed. Rigorous and critical data must be generated in a precise, timely manner to quickly evaluate and progress the compounds and the series, toward the ideal candidate profile. The higher the quality of preclinical candidates, the higher the probability of a successful progression into clinical development.

The data produced by Creative Bioarray's rapid lead optimization service play a vital role in making quick, affordable decisions around selecting and advancing the right lead candidate prior to initiating IND-enabling toxicology studies.

Creative Bioarray serves clients as an additional resource to enhance an internal team or as a fully integrated partner in a drug discovery team. Utilizing an integrated approach, we have delivered promising lead compounds in a wide range of therapeutic and target class areas, including GPCRs, ion channels, kinases, and proteases.

Lead Optimization Services

At Creative Bioarray, each lead optimization study is unique and designed on a case-by-case basis by our scientists to meet your needs. We aim to deliver important, decision-ready results in the shortest time possible. Access our lead optimization services individually or as an integrated package. Our full set of services includes:

  • Physicochemical properties

a) Solubility
b) Stability
c) Chemical/Physical characterization

  • ADME properties

a) CYP induction
b) CYP inhibition
c) Drug-drug interaction
d) Permeability
e) Plasma protein binding
f) Metabolic stability
g) Metabolite identification and profiling

  • Potential toxicity

a) Cytotoxicity
b) 3T3-NRU-phototoxicity
c) hERG screening
d) Genotoxicity screening
e) Skin absorption
f) Skin irritation
g) Skin corrosion

  • Pharmacokinetics

a) Pharmacological screening
b) Pharmacokinetics
c) Toxicology screening
d) Safety biomarkers
e) Fast and efficient development of bioanalysis methods

Working with us means benefiting from our state-of-the-art facilities, our team's extensive expertise, and mature experience over the course of dozens of successful programs. We can deliver excellent preclinical candidates, enabling your program to advance into the clinic with confidence.

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