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HTL14242 | HTL14242 : 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
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GRM5
  • pKi:9.3
  • IC50:0.6 nM
Negative Allosteric
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Cross-screened in an external panel (Eurofins) of 30 GPCR, kinase, ion-channel, and transporter targ ...

Potency
Cellular
In Vitro

GRM5

Mode of Action: Negative Allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b00892

In Vivo Validations

Rat, Dog
Dose: 5, 10, 30 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 2.3 (R), 6.5 (D) h
Systemic clearance: 27 (R, D) mL/min/Kg

DOI Reference: 10.1021/acs.jmedchem.5b00892

Orthogonal Probes def

PF470

Chemical Information

Molecular Formula C16H8ClFN4
SMILEs N#Cc1cc(Cl)cc(-c2cc(-c3ccc(F)cn3)ncn2)c1
InChI InChI=1S/C16H8ClFN4/c17-12-4-10(7-19)3-11(5-12)15-6-16(22-9-21-15)14-2-1-13(18)8-20-14/h1-6,8-9H
Molecular weight 310.04 Da
AlogP 3.869780000000002
HBond acceptors 4
HBond donors --
Atoms 30

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Expert Reviews

by SERP
(on 24 Sept 2021 )
Cellular Use Rating
In Model Organisms
It is important to note that a metal-binding motif is present in the molecule so the presence of metal in in vitro assays for example could impact results with this compound.
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