What has polar surface area ever done for drug discovery?

Novel pyrrolyl 2-aminopyridines as potent and selective human β-secretase (BACE1) inhibitors

(2010) Michael S. Malamas et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif

(2010) Laurent Hortala et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of potent, highly constrained CGRP receptor antagonists

(2010) Craig A. Stump et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist

(2010) Ian M. Bell et al.   ACS Medicinal Chemistry Letters

5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCθ: Optimization of enzymatic and functional activity

(2009) L. Nathan Tumey et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists

(2009) Ian M. Bell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood–brain penetration

(2009) Baihua Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood–brain-barrier

(2009) Jean-Marie Receveur et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase

(2008) Andrew K. Takle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and structure–activity relationship of aminopyrimidine IKK2 inhibitors

(2008) Alistair H. Bingham et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Topological Polar Surface Area: A Useful Descriptor in 2D-QSAR

(2008) S. Prasanna et al.   CURRENT MEDICINAL CHEMISTRY

The Calculation of Polar Surface Area from First Principles: An Application of Quantum Chemical Topology to Drug Design

(2007) Ian Bytheway et al.   ChemMedChem