ESCITALOPRAM

ESCITALOPRAM : Inhibitor of SLC6A4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe ESCITALOPRAM is in the process of SERP review.

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Information

SLC6A4

Inhibitor

up to 10 uM
Reviewer recommended concentration: less than 1 µM

Probe Availability:

In Vitro Validations

Uniprot ID: P31645

Target Class: Solute Carrier

Target SubClass: Serotonin transporter

Potency: Kd

Potency Value: 2.1 nM

Potency Assay: Radioligand assay

PDB ID for probe-target interaction (3D structure): 5I71, 5I73, 5I75

Target aliases:

Sodium-dependent serotonin transporter, HTT, SLC6A ...

DOI Reference: 10.1038/nature17629

Uniprot ID: P31645

Target Class: Solute Carrier

Target SubClass: Serotonin transporter

Potency: Ki

Potency Value: 0.89 nM

Potency Assay: Radioligand binding displacement

PDB ID for probe-target interaction (3D structure): 5I71, 5I73, 5I75

Target aliases:

Sodium-dependent serotonin transporter, HTT, SLC6A ...

DOI Reference: 10.1021/jm1005034

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET): Ki = 10500 nM (DAT), 8150 nM (NET)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 effects. It has PK commensurate with oral dosing in vivo.

(last updated: 18 Jan 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 in inhibiting serotonin re-uptake in the CNS. Although it is six times less potent than citalopram, it still a binder of the histamine H1(without causing observed pharmacological action) and muscarinic receptors. see doi: 10.1517/17425255.3.5.741

(last updated: 2 Feb 2023 )