SB-258719

SB-258719 : Reverse agonist of 5-HT7 receptor

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe SB-258719 is in the process of SERP review.

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Information

HTR7

Reverse agonist

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P34969

Target Class: GPCR

Target SubClass: Serotonin receptor

Potency: Ki

Potency Value: 31.6 nM

Potency Assay: Radio ligand binding assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

5-hydroxytryptamine receptor 7, HTR7, 5HT7R_HUMAN, ...

DOI Reference: 10.1021/jm970519e

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): SB-258719 displays > 100-fold selectivity over a range of other receptors (5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2A, 5-HT2B). (DOI: 10.1021/jm970519e)

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Radioligand displacement data looks promising, but receptor selectivity in cells was not confirmed.

(last updated: 30 Oct 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is the only commercially available 5HT7 antagonist, which excuses the rather modest amount of data available for it. Care should be taken regarding the potential effects on the off-targets with pKi 5.4 for D2 and D3; pKi 5.5 for 5-HT1D, respectively.

(last updated: 14 Oct 2025 )