BN-81644 | BN-81644 : Competitive antagonist of SSTR3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
In Vivo
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SSTR3
  • Ki:0.64 ± 0.12 nM
  • IC50:2.7 ± 0.7 nM
Competitive
100 nM up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: Ki 3700 nM SSTR1, Ki >10000nM SSTR2, Ki 7100 nM SSTR4 and Ki 2200 ...

Potency
Cellular
In Vitro

SSTR3

Mode of Action: Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm0108449

Chemical Information

Molecular Formula C28H34N4
SMILEs CCCCC1(CCCC)N[C@@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21
InChI InChI=1S/C28H34N4/c1-3-5-16-28(17-6-4-2)26-22(21-14-10-11-15-23(21)30-26)18-24(32-28)27-29-19-25(31-27)20-12-8-7-9-13-20/h7-15,19,24,30,32H,3-6,16-18H2,1-2H3,(H,29,31)/t24-/m1/s1
Molecular weight 426.28 Da
AlogP 0.0
HBond acceptors 4
HBond donors 3
Atoms 66

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews


(on 30 Nov 2023)
Cellular Use Rating
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...
(on 7 Jan 2024)
Cellular Use Rating
(The reviewer did not leave any public comments)
(on 14 Oct 2025)
Cellular Use Rating
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...
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