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SB-258719 | SB-258719 : Reverse agonist of 5-HT7 receptor
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HTR7
  • Ki:31.6 nM
  • EC50:20 nM
Reverse agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
SB-258719 displays > 100-fold selectivity over a range of other receptors (5-HT1A, 5-HT1B, 5-HT1D, 5 ...

Potency
Cellular
In Vitro

HTR7

Mode of Action: Reverse agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm970519e

Chemical Information

Molecular Formula C18H30N2O2S
SMILEs Cc1cccc(S(=O)(=O)N(C)[C@H](C)CCN2CCC(C)CC2)c1
InChI InChI=1S/C18H30N2O2S/c1-15-8-11-20(12-9-15)13-10-17(3)19(4)23(21,22)18-7-5-6-16(2)14-18/h5-7,14-15,17H,8-13H2,1-4H3/t17-/m1/s1
Molecular weight 338.20 Da
AlogP 3.1260200000000022
HBond acceptors 4
HBond donors --
Atoms 53

References

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Expert Reviews

by SERP
(on 30 Oct 2023 )
Cellular Use Rating
Radioligand displacement data looks promising, but receptor selectivity in cells was not confirmed.
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
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...
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