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Assay Detail

CHEMBL5626981

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

Binding
Antagonist activity at GluN1-1a/GluN2B (unknown origin) expressed in xenopus laevis oocytes assessed as inhibition of glycine/glutamate-induced channel current incubated for 20s measured at holding potential of -70 mV by two-electrode voltage clamp technique
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of triazole-bridged aryl adamantane analogs as an intriguing class of multifunctional agents for treatment of Alzheimer's disease.
Gutti G, Leifeld J, Kakarla R, Bajad NG, Ganeshpurkar A, Kumar A, Krishnamurthy S, Klein-Schmidt C, Tapken D, Hollmann M, Singh SK.
Eur J Med Chem (2023) 259 : 115670 -115670
PubMed 37515920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.78 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL807 MEMANTINE 4.0 1 6.11
CHEMBL5631356 1 5.41
CHEMBL5633239 1 5.30
CHEMBL5632076 1 4.66
CHEMBL5629932 1 4.42
CHEMBL5632160 1 4.20
CHEMBL5633141 1 4.10
CHEMBL5632219 1 4.01
CHEMBL5632181 1 -
CHEMBL5631427 1 -
CHEMBL5632465 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL807 MEMANTINE IC50 = 778.0 nM 6.11
CHEMBL5631356 IC50 = 3876.0 nM 5.41
CHEMBL5633239 IC50 = 5054.0 nM 5.30
CHEMBL5632076 IC50 = 21771.0 nM 4.66
CHEMBL5629932 IC50 = 38177.0 nM 4.42
CHEMBL5632160 IC50 = 63650.0 nM 4.20
CHEMBL5633141 IC50 = 79450.0 nM 4.10
CHEMBL5632219 IC50 = 97293.0 nM 4.01
CHEMBL5632181 IC50 = 216556.0 nM -
CHEMBL5631427 IC50 = 115634.0 nM -
CHEMBL5632465 IC50 = 196940.0 nM -