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PF470 | PF470 : Negative Allosteric Modulator of GRM5
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
GRM5
  • Ki:0.9 nM
  • IC50:2.5 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selective vs mGLU1 (IC50 = 30.5 uM), PF470 showed no apparent functional agonism (orthosteric or all ...

Potency
Cellular
In Vitro

GRM5

Mode of Action: Negative Allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm401622k

In Vivo Validations

Rat, Monkey
Dose: 1 (IV), 5-30 (PO) mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 0.31 (R), 1.4 (M) h
Systemic clearance: 52 (R), 18 (M) mL/min/Kg

DOI Reference: 10.1021/jm401622k

Orthogonal Probes def

HTL14242

Chemical Information

Molecular Formula C18H16N6O
SMILEs Cc1ccncc1-c1nn(C)c2nc(OCc3ccccn3)cnc12
InChI InChI=1S/C18H16N6O/c1-12-6-8-19-9-14(12)16-17-18(24(2)23-16)22-15(10-21-17)25-11-13-5-3-4-7-20-13/h3-10H,11H2,1-2H3
Molecular weight 332.14 Da
AlogP 2.707720000000001
HBond acceptors 7
HBond donors --
Atoms 41

References

Publications

Cross References

ChEMBL BindingDB PubChem canSAR

Vendors

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Expert Reviews

by SERP
(on 7 Apr 2025)
Cellular Use Rating
In Model Organisms
PF470 is a well-characterized negative allosteric modulator for mGluR5. Together with HTL14242 (also rated in this portal) both can be used as orthogonal chemical probes to study mGluR5 pharmacology. PF470...
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