Compound name
TP-050n
Protein family
Ion Channel
Target name
GRIN2A
Affinity on-target cellular (nM)
30000
CG-Set
Ion Channel
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001557a
SMILES
Cc1cn([C@@H](C)CC#N)c(=O)c2cc(Cn3nc(C(F)F)cc3Cl)nn12
InChIKey
BEBDKSYNJJVZSO-VIFPVBQESA-N
NCBI gene ID
2903
UniProt ID
Q12879
Synonyms
EPND, FESD, GluN2A, LKS, NMDAR2A, NR2A
Mode of action
Negative control for TP-050
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Ca2+ influx assay (using CHO cells expressing GluN2A/GluN1a in the presence of glutamate at an EC30 concentration)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/pii/S0968089621005848?via%3Dihub
Affinity on-target cellular relation
>
Selectivity remarks
Screened in Ca2+ influx assay (using CHO cells expressing NMDA receptor subtype in the presence of glutamate at an EC30 concentration): EC50(GluN2A)>30 µM, max potentiation at 30 µM <150%; AMPA binding (scintillation proximity assay (SPA) with 100 µM glutamate): IC50 >30 µM
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S0968089621005848?via%3Dihub