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Assay Detail

CHEMBL982936

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

Binding
Inhibition of NMDA NR1/NR2B receptor expressed in xenopus oocytes assessed as inhibition of NMDA and glycine-induced current response by two-electrode voltage clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Oocyte
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
Rosini M, Simoni E, Bartolini M, Cavalli A, Ceccarini L, Pascu N, McClymont DW, Tarozzi A, Bolognesi ML, Minarini A, Tumiatti V, Andrisano V, Mellor IR, Melchiorre C.
J Med Chem (2008) 51 : 4381 -4384
PubMed 18605718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.06 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478666 CARBACRINE 1 6.13
CHEMBL807 MEMANTINE 4.0 1 5.02
CHEMBL474268 1 4.89
CHEMBL473866 1 4.74
CHEMBL478667 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478666 CARBACRINE IC50 = 740.0 nM 6.13
CHEMBL807 MEMANTINE IC50 = 9520.0 nM 5.02
CHEMBL474268 IC50 = 13000.0 nM 4.89
CHEMBL473866 IC50 = 18200.0 nM 4.74
CHEMBL478667 IC50 = 30300.0 nM 4.52