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PPTN | Antagonist of P2RY14
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
P2RY14
  • IC50:0.5 nM
  • Ki:2.3 nM
  • Ki:35 nM
  • IC50:>20 uM
Antagonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
>10,000-fold selectivity over other P2RY* receptors Shows off-target activity in the GPCR scan: the ...

Potency
Cellular
In Vitro

P2RY14

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2010.12.113

In Vivo Validations

Mouse
Dose: 25 - 75 mg/kg
Route of delivery: Oral

DOI Reference: 10.1016/j.bmcl.2010.12.113

Negative Control Compounds

PPTN-NC
Notes: P2RY14 potency > 4000x less; IC50 = 4381 nM (FLIPR assay); Ki = 8614 nM (Binding assay); Ki > 100 µM (Binding assay w/ 2% HSA); Shows off-target activity in the GPCR scan: the closest hits are SIGMAR1 (Ki = 1168.69 nM), TMEM97 (Ki = 1704.51 nM) , ADRA2B (Ki = 1836.54 nM) KINOMEScan with 468 targets at 1 µM: clean

Chemical Information

Molecular Formula C29H24F3NO2
SMILEs O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1
InChI InChI=1S/C29H24F3NO2/c30-29(31,32)25-8-5-19(6-9-25)22-7-10-26-23(15-22)16-24(28(34)35)17-27(26)21-3-1-18(2-4-21)20-11-13-33-14-12-20/h1-10,15-17,20,33H,11-14H2,(H,34,35)
Molecular weight 475.18 Da
AlogP 0.0
HBond acceptors 3
HBond donors 2
Atoms 59

Vendors

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Expert Reviews

No SERP comments found for PPTN

Portal Comments

In a 2023 study, Hu et al. evaluated PPTN in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)

Probe PPTN is in the process of SERP review.

Please continue to check back for new reviews and commentary.