Compound name
TP-050
Protein family
Ion Channel
Target name
GRIN2A
Affinity on-target cellular (nM)
510
CG-Set
Ion Channel
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001556a
SMILES
Cc1cn([C@H](C)CC#N)c(=O)c2cc(Cn3nc(C(F)F)cc3Cl)nn12
InChIKey
BEBDKSYNJJVZSO-SECBINFHSA-N
NCBI gene ID
2903
UniProt ID
Q12879
Synonyms
EPND, FESD, GluN2A, LKS, NMDAR2A, NR2A
Mode of action
Positive allosteric modulator
Negative control
TP-050n
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
0
Selectivity platform
NMDA receptor panel
Selectivity platform number of targets
3
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) = 0.51 µM, max potentiation at 30 µM = 350%; EC50(GluN2B) n.d., max potentiation at 30 µM <150%, EC50(GluN2C) >30 µM, max potentiation at 30 µM = 200%, EC50(GluN2D) = 9.6 µM, max potentiation at 30 µM = 260%; AMPA binding (scintillation proximity assay, SPA, with 100 µM glutamate): IC50 >30 µM; Screened at 10 µM against 47 targets (SAFETYscan assays, DiscoverX), in-vitro potencies of targets: IC50(PDE3A) = 7.9 µM (56% inhibition), others IC50 >10 µM
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S0968089621005848?via%3Dihub
Selectivity Number of Off-targets
0