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PCS1055 | PCS1055 : Antagonist of M4 receptor
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CHRM4
  • Ki:6.53 ± 0.797 nM
  • IC50:18.1 ± 0.658 nM
Antagonist
100 nM
up to 300 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within family: 130 fold to M1, 31.2 fold to M2, 426 fold to M3, 1580 fold to M5 in in vi ...

Potency
Cellular
In Vitro

CHRM4

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.ejphar.2016.04.022

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1016/j.ejphar.2016.04.022

Orthogonal Probes def

PD-102807

Chemical Information

Molecular Formula C27H32N4
SMILEs c1ccc(CN2CCC(CCNc3cc4c(nn3)-c3ccccc3CCC4)CC2)cc1
InChI InChI=1S/C27H32N4/c1-2-7-22(8-3-1)20-31-17-14-21(15-18-31)13-16-28-26-19-24-11-6-10-23-9-4-5-12-25(23)27(24)30-29-26/h1-5,7-9,12,19,21H,6,10-11,13-18,20H2,(H,28,29)
Molecular weight 412.26 Da
AlogP 5.346500000000005
HBond acceptors 4
HBond donors 1
Atoms 63

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 17 Nov 2023 )
Cellular Use Rating
In Model Organisms
This is a reasonably selective, and potent (6nM) M4 antagonist - selectivity for M4 is difficult to achieve, so this in itself makes this worth considering. It is well characterised pharmacologically...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
This could be a good in cell probe for the target, however, insufficient selectivity data against unrelated targets has been presented (although there is mention of this being conducted). At the dose...
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