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Assay Detail

CHEMBL4149863

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Forebrain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL311)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Marcin LR, Warrier J, Thangathirupathy S, Shi J, Karageorge GN, Pearce BC, Ng A, Park H, Kempson J, Li J, Zhang H, Mathur A, Reddy AB, Nagaraju G, Tonukunuru G, Gupta GVRKM, Kamble M, Mannoori R, Cheruku S, Jogi S, Gulia J, Bastia T, Sanmathi C, Aher J, Kallem R, Srikumar BN, Vijaya KK, Naidu PS, Paschapur M, Kalidindi N, Vikramadithyan R, Ramarao M, Denton R, Molski T, Shields E, Subramanian M, Zhuo X, Nophsker M, Simmermacher J, Sinz M, Albright C, Bristow LJ, Islam I, Bronson JJ, Olson RE, King D, Thompson LA, Macor JE.
ACS Med Chem Lett (2018) 9 : 472 -477
PubMed 29795762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.37 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4111330 1 8.85
CHEMBL4115628 1 8.85
CHEMBL3892956 1 8.40
CHEMBL4115649 1 8.37
CHEMBL4170867 1 8.36
CHEMBL4168402 1 8.11
CHEMBL4161899 1 8.08
CHEMBL3911371 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4111330 Ki = 1.4 nM 8.85
CHEMBL4115628 Ki = 1.4 nM 8.85
CHEMBL3892956 Ki = 4.0 nM 8.40
CHEMBL4115649 Ki = 4.3 nM 8.37
CHEMBL4170867 Ki = 4.4 nM 8.36
CHEMBL4168402 Ki = 7.7 nM 8.11
CHEMBL4161899 Ki = 8.4 nM 8.08
CHEMBL3911371 Ki = 11.0 nM 7.96