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AMG-PERK-44 | AMG-PERK-44 : 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
  • IC50:6 nM
  • IC50:84 nM
  • IC50:770 nM
  • EC50:400 nM
Inhibitor
10 mg/kg for in vivo use
1 µM

Selectivity

In Vitro Selectivity Assessment
EIF2AK4

Gene ID: Q9P2K8

Organism: Homo sapiens

Family: Ser/Thr protein kinase family

Potency: IC50 - 7300 nM

Potency Assay Off-Target:
TR-FRET assay (using 120 µM ATP (= 0.66 x Km), Cisbio Inc.)
Selectivity Assessment Description:
Screened at 1 µM against 387 kinases, KINOMEscan (DiscoveRx). Clean selectivity profile, no target w ...

Potency
Cellular
In Vitro

EIF2AK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm5017494

In Vivo Validations

Mouse
Dose: 2.5 mg/kg
Route of delivery: Oral
Plasma half life: MRT = 5.0 h
Area Under the Curve:: 1.4 µM x h
Fb : 55%
Volume of Distribution at Steady-State: 3.6 L/kg
Target engagement assay: Compounds dosed in male CD-1 mice as a solution at 2.5 mg/kg po in 1% Pluronic F68/1% HPMC/15% Captisol/83% H2O, pH 2.0, with MsOH.

DOI Reference: 10.1021/jm5017494

Orthogonal Probes def

CANSAR384279

Chemical Information

Molecular Formula C34H28N4O2
SMILEs Cc1ccc2cc(-c3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)ccc2n1
InChI InChI=1S/C34H28N4O2/c1-21-14-18-27(31(35)29(21)25-17-19-28-24(20-25)16-15-22(2)36-28)33(39)30-32(23-10-6-4-7-11-23)37(3)38(34(30)40)26-12-8-5-9-13-26/h4-20H,35H2,1-3H3
Molecular weight 524.22 Da
AlogP 6.48824
HBond acceptors 6
HBond donors 2
Atoms 68
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Vendors

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Expert Reviews

by SERP
(on 21 Oct 2024 )
Cellular Use Rating
In Model Organisms
Compound 44 exhibits impressive potency and selectivity as an inhibitor of PERK, making it a valuable tool for elucidating PERK’s role in cellular signaling. Notably, Compound 44 offers chemical diversity...
by SERP
(on 26 Nov 2024 )
Cellular Use Rating
In Model Organisms
AMG-PERK-44 is an excellent chemical probe for PERK, with absolute selectivity for PERK relative to >370 other kinases and a structurally validated ATP-competitive binding mode. AMG-PERK-44 is the most...
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