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ESCITALOPRAM | ESCITALOPRAM : Inhibitor of SLC6A4
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
SLC6A4
  • Kd:2.1 nM
  • Ki:0.89 nM
  • Activity:89-3% residual activity
Inhibitor
less than 1 µM
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET): Ki = 10500 nM ...

Potency
Cellular
In Vitro

SLC6A4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nature17629

In Vivo Validations

Rat
Dose: 1.6 mg/Kg
Route of delivery: Subcutaneous
Plasma half life: 54 min
Cmax: 131 nM
Tmax: 26 min
Area Under the Curve:: 13,888 nM*min
Fb : 50%

DOI Reference: 10.1124/dmd.112.045682

Chemical Information

Molecular Formula C20H21FN2O
SMILEs CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21
InChI InChI=1S/C20H21FN2O/c1-23(2)11-3-10-20(17-5-7-18(21)8-6-17)19-9-4-15(13-22)12-16(19)14-24-20/h4-9,12H,3,10-11,14H2,1-2H3/t20-/m0/s1
Molecular weight 324.16 Da
AlogP 3.812980000000003
HBond acceptors 3
HBond donors --
Atoms 45

References

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Cross References

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Expert Reviews

by SERP
(on 18 Jan 2023 )
Cellular Use Rating
In Model Organisms
Escitalopram is a highly potent and selective SERT inhibitor drug. It is also a relatively lipophilic basic compound. High concentrations should not be required to probe SERT biology and may lead to polypharmacological...
by SERP
(on 2 Feb 2023 )
Cellular Use Rating
In Model Organisms
Escitalopram, the active (S)-enantiomer of citalopram, has been approved for the treatment of depression and anxiety disorders for many years. It is more potent and selective than the racemate citalopram...
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