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Assay Detail

CHEMBL744927

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

Binding
Inhibition of [3H]MK-801 binding to NMDA receptor of rat cerebral cortical synaptic membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

(+/-)-(Z)-2-(aminomethyl)-1-phenylcyclopropanecarboxamide derivatives as a new prototype of NMDA receptor antagonists.
Shuto S, Takada H, Mochizuki D, Tsujita R, Hase Y, Ono S, Shibuya N, Matsuda A.
J Med Chem (1995) 38 : 2964 -2968
PubMed 7636857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.80 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99946 LEVOMILNACIPRAN 4.0 1 5.20
CHEMBL316566 1 5.00
CHEMBL98994 1 4.89
CHEMBL11 IMIPRAMINE 4.0 1 4.85
CHEMBL100561 1 4.06
CHEMBL101447 1 -
CHEMBL318462 1 -
CHEMBL317169 1 -
CHEMBL99947 1 -
CHEMBL101715 1 -
CHEMBL318506 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99946 LEVOMILNACIPRAN IC50 = 6300.0 nM 5.20
CHEMBL316566 IC50 = 10000.0 nM 5.00
CHEMBL98994 IC50 = 13000.0 nM 4.89
CHEMBL11 IMIPRAMINE IC50 = 14000.0 nM 4.85
CHEMBL100561 IC50 = 88000.0 nM 4.06
CHEMBL101447 IC50 > 100000.0 nM -
CHEMBL318462 IC50 > 100000.0 nM -
CHEMBL317169 IC50 > 100000.0 nM -
CHEMBL99947 IC50 > 100000.0 nM -
CHEMBL101715 IC50 > 100000.0 nM -
CHEMBL318506 IC50 > 100000.0 nM -