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SBP-3264 | SBP-3264 : Inhibitor of STK3, STK4
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
STK3
  • IC50:4 nM
  • Kd:13 nM
  • IC50:139 ± 19 nM
  • IC50:3.700 - 10600 nM
STK4
  • IC50:15 nM
  • Kd:11 nM
  • IC50:122 ± 7
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinase selectivity of cpd 20 at 1.0 μM was determined against a panel of 468 kinases using the KINOM ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selecivity of cpd 20 against BMP2K, ULK3, LKB1, and AURKA was assessed using the NanoBRET intracellu ...

Potency
Cellular
In Vitro

STK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00804

STK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00804

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 5.3 h
Cmax: 11.8 uM
Tmax: 0.25 h
Area Under the Curve:: 8.1 μmol/L/h

DOI Reference: 10.1021/acs.jmedchem.1c00804

Negative Control Compounds

cpd 9
SMILES: CC(C=C1)=CC=C1C2=CNC3=NC=NC(N4CCOCC4)=C32

Chemical Information

Molecular Formula C19H20ClN5O
SMILEs CC(=O)NC1CCN(c2ncnc3[nH]cc(-c4cccc(Cl)c4)c23)CC1
InChI InChI=1S/C19H20ClN5O/c1-12(26)24-15-5-7-25(8-6-15)19-17-16(10-21-18(17)22-11-23-19)13-3-2-4-14(20)9-13/h2-4,9-11,15H,5-8H2,1H3,(H,24,26)(H,21,22,23)
Molecular weight 369.14 Da
AlogP 3.3832000000000013
HBond acceptors 6
HBond donors 2
Atoms 46

Expert Reviews

No SERP comments found for SBP-3264

Probe SBP-3264 is in the process of SERP review.

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