The Explora ADMET Services consist of a range of in vitro assays that are tailored toward incorporating early ADMET information into Medicinal Chemistry efforts, and can now be offered also as as a standalone service. An updated 2008 brochure including a price list and full detailed protocols, is available for download.

 

In Vivo Pharmacokinetics

A series of non-GLP in vivo assays tailored to provide a preliminary pharmacokinetic information of promising leads are also available. They include pharmacokinetic evaluation in rats and mice; disposition and distribution of compounds in tissues and organs (e.g., brain penetration) and biotransformation analysis. An updated 2008 brochure, including a price list and full detailed protocols, is accessible.

NiKem Research Services: Focused on Drug Discovery

Early ADMET and in vivo PK Services

Explora ADMET: Reveal and Focus Assays

The Reveal Assays are a collection of basic, essential in vitro assays for the quick identification of the important developability information that helps guide the lead optimization process. The Focus Assays are available to probe developability parameters in finer detail when needed, for example in the later stages of lead optimization or when a promising class of compounds exhibited unfavourable results from the initial Reveal Assays.

 

Reveal Assays

Focus Assays
CYP 450 Inhibition
(1A2, 2D6, 2C9, 2C19, 3A42B6-NEW!, 2E1-NEW!, 2C8-NEW!, 3A5-NEW!)		 % inhibition IC50
CYP450 Phenotyping – NEW! (1A2, 2D6, 2C9, 2C19, 3A4) % inhibition Half-life
Time-dependent CYP3A4 inhibition – NEW!   IC50
Metabolic Stability % Remaining in plasma and liver microsomes of multiple species

Half-life in plasma, liver microsomes and hepatocytes of multiple species

Biotransformation analysis

Intestinal Permeability
(PAMPA, Caco-2)

BBB Permeability
(PAMPA, MDCK-hMDR1)

 A-B determination

A-B / B-A determination

A-B / B-A with PGP inhibitors
Solubility Dilution DMSO solution Shake-flask
Cellular Toxicity LD50 in HepG2 cells LD50 in HepG2 cells and rat hepatocytes
Simulated Gastric/Intestinal Fluid Stability - NEW! % remaining in SGF or SIF  
hERG Binding % inhibition Ki
Plasma Protein Binding % bound, ultrafiltration, or equilibrium
dialysis - NEW!