PF-06263276

Ligand id: 9432

Name: PF-06263276

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 3
Rotatable bonds 6
Topological polar surface area 126.92
Molecular weight 566.26
XLogP 5.55
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Bioactivity Comments
In vitro and in vivo potencies, and the pharmacokinetic and safety profiles of PF-06263276 indicate suitability for inhaled or topical therapy to treat inflammatory diseases, such as COPD or psoriasis, through direct administration to the lungs or skin, thus avoiding any systemic effects of JAK inhibition [1]. IC50 evaluation was performed at 100nM ATP.
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Janus kinase 1 Hs Inhibitor Inhibition 8.7 pIC50 - 1
pIC50 8.7 (IC50 2.2x10-9 M) [1]
Janus kinase 2 Hs Inhibitor Inhibition 7.6 pIC50 - 1
pIC50 7.6 (IC50 2.31x10-8 M) [1]
tyrosine kinase 2 Hs Inhibitor Inhibition 7.5 pIC50 - 1
pIC50 7.5 (IC50 2.97x10-8 M) [1]
Janus kinase 3 Hs Inhibitor Inhibition 7.2 pIC50 - 1
pIC50 7.2 (IC50 5.99x10-8 M) [1]