Chemical Probes logo

PPTN

Antagonist of P2RY14

Structure

Information

  • P2RY14
  • Antagonist
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q15391
Target Class: GPCR
Target SubClass: Purinergic Receptor
Potency: IC50
Potency Value: 0.5 nM
Potency Assay: FLIPR assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
P2Y purinoceptor 14, KIAA0001, GPR105, P2RY14, P2Y ...

DOI Reference: 10.1016/j.bmcl.2010.12.113

Uniprot ID: Q15391
Target Class: GPCR
Target SubClass: Purinergic Receptor
Potency: Ki
Potency Value: 2.3 nM
Potency Assay: Binding assay (no HSA)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
P2Y purinoceptor 14, KIAA0001, GPR105, P2RY14, P2Y ...

DOI Reference: 10.1016/j.bmcl.2010.12.113

Uniprot ID: Q15391
Target Class: GPCR
Target SubClass: Purinergic Receptor
Potency: Ki
Potency Value: 35 nM
Potency Assay: Binding assay with 2% HSA
PDB ID for probe-target interaction (3D structure): --
Target aliases:
P2Y purinoceptor 14, KIAA0001, GPR105, P2RY14, P2Y ...

DOI Reference: 10.1016/j.bmcl.2010.12.113

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
>10,000-fold selectivity over other P2RY* receptors Shows off-target activity in the GPCR scan: the closest hits are DRD3 (Ki = 884.3 nM), TMEM97 (Ki = 1120.99 nM) , SIGMAR1 (Ki = 1180.59 nM), ADRA2B (Ki = 2561.53 nM) Outside Target Family: Closest off-targets (Panlabs): CYSLTR1 (h): IC50 = 560 nM @ 1µM, HRH2 (h): IC50 = 1390 nM @ 10 µM, SLC6A3 (Dopamine Transporter) (h): IC50 = 2310 nM @ 10 µM
I have extra information to add

SERP ratings and comments

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)