PF-06650833

Ligand id: 9667

Name: PF-06650833

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 103.54
Molecular weight 361.14
XLogP 2
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

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

Bioactivity Comments
PF-06650833 inhibits TLR7/8 agonist R848-induced TNFα production in human peripheral blood mononuclear cells with an IC50 of 2nM [1]. Further preclinical results detailing the pharmacokinetic and ADME profiles of PF-06650833 are reported in [1]. In a kinome selectivity profile 200nM PF-06650833 completely inhibited IRAK4 activity, and inhibited the additional kinases IRAK1, MNK2, LRRK2, CLK4, and CK1γ1 by > 70%. In a more physiologically relevant screen, other than IRAK4, 200nM PF-06650833 inhibited only CK1γ2, IRAK3/M, PIPK2C, and CK1δ/ε by > 50%.
Selectivity at enzymes
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
interleukin 1 receptor associated kinase 4 Hs Inhibitor Inhibition 9.7 pIC50 - 1
pIC50 9.7 (IC50 2x10-10 M) [1]