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GSK2656157 | GSK2656157 : Inhibitor of EIF2AK3
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
EIF2AK3
  • IC50:0.8 nM
  • IC50:10-30 nM
  • IC50:30 nM
Inhibitor
100 nM to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinase selectivity was evaluated using 27 kinases at GSK as well as a panel of 300 kinases at Reacti ...

Potency
Cellular
In Vitro

EIF2AK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml400228e

In Vivo Validations

Mouse
Dose: 2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.25 h
Systemic clearance: 10.5 mL/min/Kg
Area Under the Curve:: 3270 ng*h/mL
Volume of Distribution at Steady-State: 0.72 L/Kg

DOI Reference: 10.1021/ml400228e

Dose: 13.4 mg/Kg
Route of delivery: Oral
Area Under the Curve:: 13378.6 ng*h/mL
Bioavailability: 52%

DOI Reference: 10.1021/ml400228e

Rat
Dose: 2.2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.4 h
Systemic clearance: 9.5 mL/min/Kg
Area Under the Curve:: 3931.0 ng*h/mL
Volume of Distribution at Steady-State: 0.6 L/Kg

DOI Reference: 10.1021/ml400228e

Dose: 4.3 mg/Kg
Route of delivery: Oral
Area Under the Curve:: 8015.7 ng*h/mL
Bioavailability: 100%

DOI Reference: 10.1021/ml400228e

Dog
Dose: 2.9 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.1 h
Systemic clearance: 15.5 mL/min/Kg
Area Under the Curve:: 3128.5 ng*h/mL
Volume of Distribution at Steady-State: 2.8 L/Kg

DOI Reference: 10.1021/ml400228e

Dose: 5.2 mg/Kg
Route of delivery: Oral
Area Under the Curve:: 6210.0 ng*h/mL
Bioavailability: 100%

DOI Reference: 10.1021/ml400228e

Negative Control Compounds

CANSAR203754
Notes: cpd 4 - IC50 63 nM in vitro, no activity in cell

Chemical Information

Molecular Formula C23H21FN6O
SMILEs Cc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
InChI InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27)
Molecular weight 416.18 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 52

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 23 Oct 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 26 Oct 2022 )
Cellular Use Rating
In Model Organisms
GSK2656157 is selective inhibitor of PERK kinase (EIF2AK3) that binds the nucleotide pocket. In terms of selectivity in binding potency, it is at least 500-fold selective over other members of the EIF2AK...
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