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Assay Detail

CHEMBL3241939

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

Binding
Potentiation of rat recombinant GluN1/GluN2C expressed in Xenopus laevis oocytes assessed as increase in glutamate/glycine-induced current response by two-electrode voltage clamp technique relative to control
37
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; Grin1/Grin2c (CHEMBL2096911)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators.
Zimmerman SS, Khatri A, Garnier-Amblard EC, Mullasseril P, Kurtkaya NL, Gyoneva S, Hansen KB, Traynelis SF, Liotta DC.
J Med Chem (2014) 57 : 2334 -2356
PubMed 24512267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 4.76 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237286 1 5.37
CHEMBL3237289 1 5.16
CHEMBL3237250 1 5.16
CHEMBL3237287 1 5.10
CHEMBL3237291 1 5.09
CHEMBL3237285 1 5.07
CHEMBL3237253 1 5.06
CHEMBL3237257 1 5.05
CHEMBL3237292 1 5.01
CHEMBL3237254 1 4.96
CHEMBL3237256 1 4.92
CHEMBL3237294 1 4.89
CHEMBL3237293 1 4.89
CHEMBL3237284 1 4.89
CHEMBL3237301 1 4.85
CHEMBL3237275 1 4.82
CHEMBL3237260 1 4.82
CHEMBL3237281 2 4.80
CHEMBL3237268 1 4.80
CHEMBL3237252 1 4.80
CHEMBL3237249 1 4.77
CHEMBL3237288 1 4.75
CHEMBL478141 1 4.62
CHEMBL3237246 1 4.62
CHEMBL3237290 1 4.60
CHEMBL3237270 1 4.54
CHEMBL3237277 1 4.46
CHEMBL3237278 1 4.44
CHEMBL3237279 1 4.43
CHEMBL3237298 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237286 EC50 = 4300.0 nM 5.37
CHEMBL3237289 EC50 = 7000.0 nM 5.16
CHEMBL3237250 EC50 = 7000.0 nM 5.16
CHEMBL3237287 EC50 = 8000.0 nM 5.10
CHEMBL3237291 EC50 = 8200.0 nM 5.09
CHEMBL3237285 EC50 = 8500.0 nM 5.07
CHEMBL3237253 EC50 = 8700.0 nM 5.06
CHEMBL3237257 EC50 = 8900.0 nM 5.05
CHEMBL3237292 EC50 = 9700.0 nM 5.01
CHEMBL3237254 EC50 = 11000.0 nM 4.96
CHEMBL3237256 EC50 = 12000.0 nM 4.92
CHEMBL3237284 EC50 = 13000.0 nM 4.89
CHEMBL3237293 EC50 = 13000.0 nM 4.89
CHEMBL3237294 EC50 = 13000.0 nM 4.89
CHEMBL3237301 EC50 = 14000.0 nM 4.85
CHEMBL3237260 EC50 = 15000.0 nM 4.82
CHEMBL3237275 EC50 = 15000.0 nM 4.82
CHEMBL3237252 EC50 = 16000.0 nM 4.80
CHEMBL3237281 EC50 = 16000.0 nM 4.80
CHEMBL3237268 EC50 = 16000.0 nM 4.80
CHEMBL3237249 EC50 = 17000.0 nM 4.77
CHEMBL3237288 EC50 = 18000.0 nM 4.75
CHEMBL3237281 EC50 = 18000.0 nM 4.75
CHEMBL3237246 EC50 = 24000.0 nM 4.62
CHEMBL478141 EC50 = 24000.0 nM 4.62
CHEMBL3237290 EC50 = 25000.0 nM 4.60
CHEMBL3237270 EC50 = 29000.0 nM 4.54
CHEMBL3237277 EC50 = 35000.0 nM 4.46
CHEMBL3237278 EC50 = 36000.0 nM 4.44
CHEMBL3237279 EC50 = 37000.0 nM 4.43
CHEMBL3237298 EC50 = 37000.0 nM 4.43
CHEMBL3237295 EC50 = 40000.0 nM 4.40
CHEMBL3237276 EC50 = 46000.0 nM 4.34
CHEMBL3237248 EC50 = 52000.0 nM 4.28
CHEMBL3237300 EC50 = 52000.0 nM 4.28
CHEMBL3237247 EC50 = 61000.0 nM 4.21
CHEMBL3237302 EC50 = 105000.0 nM -