Technical Notes

Cell Viability Assessment

Cell viability or cytotoxicity assessments are based on cellular functions that are particularly sensitive to toxic drugs and as such provide convenient in vitro high-throughput screens (HTS) for comparing relative toxicities of a drug....

Caco-2 Permeability

The human colon epithelial cancer cell line, Caco-2, is used as a model of human intestinal absorption of drugs. This model is suitable to test compound suitability for oral dosing, predict intestinal permeability and...

Chemical Stability

The measurement of the stability of a drug in conditions that mimic the gastrointestinal tract, physiological conditions and/or in vitro biological conditions helps in identifying and understanding the lability of molecules due to non-enzymatic...

Cytochrome P450 Inhibition (Reversible)

The cytochrome P450 (CYP450) enzymes play a significant role in the metabolism of both endogenous and exogenous compounds. Within this family, CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 are predominantly involved in the...

Hepatocyte Metabolic Stability

The liver is the major site of drug metabolism in the body, with well over 50 % of marketed drugs are eliminated via hepatic mediated metabolism. Hence, measurement of the rate of clearance and...

LogD (Micro Shake-Flask)

Lipophilicity (distribution coefficient) is an important physicochemical property of a drug as it provides an understanding of how well a drug will cross lipid membranes (and thereby penetrate tissues), how well a drug will...

Microsomal Protein Binding

Understanding the non-specific binding of drugs to microsomal protein and fuinc is beneficial in generating an accurate prediction of in vivo clearance and drug-drug interactions. The leading approach for assessing microsomal protein binding is...

Microsomal Metabolic Stability

The liver is the major site of drug metabolism in the body, with well over 50% of marketed drugs being eliminated via hepatic mediated metabolism.  Hence, measurement of the rate of clearance and the...

MRP2 Inhibition

Multidrug resistant associated protein 2 (MRP2; ABCC2) is member of a family of ATP-binding cassette drug efflux transporters located in the cannalicular (apical) membrane of hepatocytes. Loss of function mutations of this transporter have...

Plasma Protein Binding

Drugs may bind to a wide variety of plasma proteins, including albumin, and the degree of binding can impact on the pharmacokinetics and pharmacodynamics parameters of a drug, given that only the free drug...

Plasma Stability

The measurement of the stability of a new chemical entity in a matrix such as plasma helps in identifying and understanding the lability of known structural moieties (e.g. amides, sulphonamide, esters, lactones, lactams to...

Tubidimetric Solubility

Low solubility can be a major obstacle during drug discovery and development, as low solubility can impact the generation of quality in vitro DMPK or biology data, can cause issues in the generation of...