Drug Target Review

APRIL 7, 2025

The challenge of GPCR drug discovery G protein-coupled receptors (GPCRs) are one of the most desirable and challenging target classes in drug discovery, as their mutation can lead to a wide range of diseases such as cancer, cardiovascular disorders and neurological conditions.

Fragment Screening 52

Fragment Screening Drugs Small Molecule Biophysical Assays 52

Drug Hunter

AUGUST 21, 2023

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Prodrugs Remain in “Proof-of-Concept” Stages Prodrug strategies for CNS deliver have also been applied with varying success , with the most famous example being L-Dopa for Parkinson’s disease. Figure 18.

Drugs 206

Drugs Disease Targeted Protein Degradation Screening Hits 206

Practical Cheminformatics

AUGUST 3, 2023

It is quite a bit more potent than the values one finds with screening hits, which typically have IC50s in the single to double-digit µM range. The ability of a compound to enter the CNS can also be facilitated or hindered by certain disease states. 200nM is an odd choice for an activity cutoff.

Drugs 84

Drugs Biochemical Assays Metabolic Stability Screening Hits 84

The ChEMBL-og

SEPTEMBER 1, 2021

Infectious disease is a leading cause of death globally and bioactivity data against pathogens (fungi, bacteria, viruses, and parasites) is an important category in ChEMBL, especially in light of the ongoing pandemic. So far, 100 K activities (against ~ 24 K compounds) have been provided through CO-ADD.

Cell Based Assays 52

Cell Based Assays Screening Hits Small Molecule Virus 52