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LP-935509 | LP-935509 : ATP competitive inhibitor of AAK1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
AAK1
  • IC50:3.3 ± 0.7 nM
  • Ki:0.9 nM
  • IC50:2.8 ± 0.4 nM
ATP competitive
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
LP-935509 effects on the kinase activity of the two most closely related kinases, BIKE and GAK (77% ...

Potency
Cellular
In Vitro

AAK1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? No

DOI Reference: 10.1124/jpet.116.235333

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 3.6 h
Cmax: 5.2 uM
Tmax: 0.5 h
Bioavailability: ~100%

DOI Reference: 10.1124/jpet.116.235333

Rat
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 4 h
Cmax: 3.1 uM
Tmax: 1.3 h
Bioavailability: 50%

DOI Reference: 10.1124/jpet.116.235333

Orthogonal Probes def

CANSAR3148788

Chemical Information

Molecular Formula C20H24N6O3
SMILEs COc1ncccc1-c1cnn2ccc(N3CCN(C(=O)OC(C)C)CC3)nc12
InChI InChI=1S/C20H24N6O3/c1-14(2)29-20(27)25-11-9-24(10-12-25)17-6-8-26-18(23-17)16(13-22-26)15-5-4-7-21-19(15)28-3/h4-8,13-14H,9-12H2,1-3H3
Molecular weight 396.19 Da
AlogP 2.4669
HBond acceptors 9
HBond donors --
Atoms 53

References

Publications

Cross References

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Expert Reviews

by SERP
(on 24 May 2023 )
Cellular Use Rating
In Model Organisms
A potent inhibitor in cells and suitable for in vivo use. While generally selective, there are noted off targets and care should be taken to make sure any new pharmacology is not caused by off target kinases...
by SERP
(on 12 Jun 2023 )
Cellular Use Rating
In Model Organisms
This inhibitor should be used carefully and data confirmed with genetic knock-down and/or knock-out. If an orthogonal inhibitor is available, it should be used in parallel. Extra caution is necessary...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria