JNJ-7891118

JNJ-7891118 : Negative Allosteric of GRIN2A

Structure

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Information

GRIN2A

Negative Allosteric

up to 10 uM

In Vitro Validations

Uniprot ID: Q12879

Target Class: Ion Channel

Target SubClass: glutamate-gated ion channel

Potency: IC50

Potency Value: 40 nM

Potency Assay: Fluorometric calcium mobilization assays (FLIPR)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Glutamate receptor ionotropic, NMDA 2A, GRIN2A, NM ...

DOI Reference: 10.1021/acs.jmedchem.4c02751

Uniprot ID: Q12879

Target Class: Ion Channel

Target SubClass: glutamate-gated ion channel

Potency: Ki

Potency Value: 78 nM

Potency Assay: Radioligand displacement assay in rat hippocampal neuron membranes

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Glutamate receptor ionotropic, NMDA 2A, GRIN2A, NM ...

DOI Reference: 10.1111/bph.70069

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): > 200 fold selectivity over other homomeric GluN2 family members: GRIN2B, GRIN2C, GRIN2D all IC50 > 50 µM (FLIPR)

Potency assay (off target): Cerep panel (Receptors, Transporters, Ion-Channels) 77 targets at 10 µM: clean; Kinase panel (373 targets, Cerep) at 1 µM: clean

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