TP-050

TP-050 : Positive allosteric of GRIN2A

Structure

SERP Rating

Probe TP-050 is in the process of SERP review.

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Information

GRIN2A

Positive allosteric

up to 30 uM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): Good NMDA-subtype selectivity (Ca2+ influx assay using CHO cells): GRIN2B EC50 > 30 µM, max potentiation < 150 %; > 59-fold selectivity; GRIN2C EC50 > 30 µM, max potentiation < 200 %; GRIN2D EC50 = 9.6 µM, max potentiation < 260 %; 19-fold selectivity; AMPA receptor scintillation proximity (SPA) binding assay: IC50 > 30 µM

Potency assay (off target): Selectivity outside target family: SAFETYscan (DiscoverX, 47 targets at 10 µM): 46 target > 10 µM; PDE3A 7.9 μM, 56% inhibition

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SERP ratings and comments

No SERP comments found for TP-050