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KW-6356 | KW-6356 : Inverse agonist of ADORA2A
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
ADORA2A
  • Kd:0.13 nM
  • Ki:0.12 nM
Inverse Agonist
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
In vitro binding assays using selective radioactively labeled ligands with 10 µM of KW-6356 were per ...

Potency
Cellular
In Vitro

ADORA2A

Mode of Action: Inverse Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1124/molpharm.122.000633

Orthogonal Probes def

IMARADENANT
MRS-1754

Chemical Information

Molecular Formula C20H19N3O4S
SMILEs Cc1ccc(C(=O)Nc2nc(-c3ccco3)c(C(=O)C3CCOCC3)s2)cn1
InChI InChI=1S/C20H19N3O4S/c1-12-4-5-14(11-21-12)19(25)23-20-22-16(15-3-2-8-27-15)18(28-20)17(24)13-6-9-26-10-7-13/h2-5,8,11,13H,6-7,9-10H2,1H3,(H,22,23,25)
Molecular weight 397.11 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 47

Expert Reviews

by SERP
(on 9 Jan 2024 )
Cellular Use Rating
KW-6356 (also known as Sipagladenant) has excellent potency against Adenosine A2A (mouse/rat/dog/marmoset/human pKi of 9.49/10.0/9.55/9.95/9.93 respectively). It shows good selectivity between Adenosine...
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