BN-81644

BN-81644 : Competitive antagonist of SSTR3

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

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.

Information

SSTR3

Competitive

100 nM up to 1 uM

Probe Availability:

Mcule

In Vitro Validations

Uniprot ID: P32745

Target Class: GPCR

Target SubClass: Somatostatin receptor

Potency: Ki

Potency Value: 0.64 ± 0.12 nM

Potency Assay: Radioligand binding assay

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

Target aliases:

Somatostatin receptor type 3, SSTR3, SSR3_HUMAN, S ...

DOI Reference: 10.1021/jm0108449

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Ki 3700 nM SSTR1, Ki >10000nM SSTR2, Ki 7100 nM SSTR4 and Ki 2200 nM SSTR5

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Although this compound is very potent and selective for sst3 compared to sst1, 2, 4 and 5, there is no broader selectivity data published so it should be used with caution in cells and perhaps as an alternative orthogonal probe only.

(last updated: 30 Nov 2023 )

SERP Ratings

In Cell Rating

(last updated: 7 Jan 2024 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

The compound shows functional potency and selectivity against closely related homologs. However, it has not been tested against unrelated targets or a broader GPCR panel. No negative control or cytotoxicity data available.

(last updated: 14 Oct 2025 )