staurosporine

Ligand id: 346

Name: staurosporine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 2
Topological polar surface area 69.45
Molecular weight 466.2
XLogP 6.05
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
Staurosporine inhibits PKCs from the cell membrane fraction with an IC50 of 1.3nM [2]. The IC50 for cytosol derived PKC inhibition is 16.3nM in the same study.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
M1 receptor Hs Allosteric modulator Positive 5.9 pKd - 8
pKd 5.9 [8]
M4 receptor Hs Allosteric modulator Neutral 5.3 pKd - 8
pKd 5.3 [8]
M2 receptor Hs Allosteric modulator Positive 5.1 pKd - 8
pKd 5.1 [8]
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
calcium/calmodulin-dependent protein kinase II beta subunit Hs Inhibitor Inhibition >10.0 pIC50 - 6
pIC50 >10.0 (IC50 <1x10-10 M) [6]
phosphorylase kinase catalytic subunit gamma 2 Hs Inhibitor Inhibition 10.0 pIC50 - 6
pIC50 10.0 (IC50 1x10-10 M) [6]
serine/threonine kinase 3 Hs Inhibitor Inhibition 9.4 pIC50 - 6
pIC50 9.4 (IC50 4.1x10-10 M) [6]
death associated protein kinase 1 Hs Inhibitor Inhibition 9.3 pIC50 - 6
pIC50 9.3 (IC50 5x10-10 M) [6]
protein kinase N1 Hs Inhibitor Inhibition 9.0 pIC50 - 6
pIC50 9.0 (IC50 1x10-9 M) [6]
mitogen-activated protein kinase kinase 4 Hs Inhibitor Inhibition >9.0 pIC50 - 10
pIC50 >9.0 (IC50 <1x10-9 M) [10]
mitogen-activated protein kinase kinase 6 Hs Inhibitor Inhibition >9.0 pIC50 - 10
pIC50 >9.0 (IC50 <1x10-9 M) [10]
p21 (RAC1) activated kinase 2 Hs Inhibitor Inhibition 9.0 pIC50 - 6
pIC50 9.0 (IC50 1x10-9 M) [6]
TRAF2 and NCK interacting kinase Hs Inhibitor Inhibition 8.9 pIC50 - 7
pIC50 8.9 (IC50 1.4x10-9 M) [7]
protein kinase, cAMP-dependent, catalytic, beta subunit Hs Inhibitor Inhibition 7.5 pIC50 - 4
pIC50 7.5 (IC50 3.3x10-8 M) [4]
protein kinase C iota Hs Inhibitor Inhibition 6.5 pIC50 - 11
pIC50 6.5 (IC50 3.46x10-7 M) [11]
homeodomain interacting protein kinase 1 Hs Inhibitor Inhibition 5.6 pIC50 - 6
pIC50 5.6 (IC50 2.639x10-6 M) [6]
Ligand mentioned in the following text fields