PMID

Data

Article Title

Organization

Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.

Pfizer

Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.

Amgen

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.

Astex Pharmaceuticals

Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

Universit£

In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.

Astrazeneca

Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.

Novartis Institutes For Biomedical Research

Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.

Amgen

Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.

Schering-Plough Research Institute

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.

Amgen

Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease.

TBA

Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

TBA

Novel Chemical Series of 5-Lipoxygenase-Activating Protein Inhibitors for Treatment of Coronary Artery Disease.

TBA

The human bile salt export pump: characterization of substrate specificity and identification of inhibitors.

King'S College Hospital

Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.

Merck

A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

Amgen

Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.

Astrazeneca