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

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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 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...
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