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Assay Detail

CHEMBL3373058

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

Binding
Displacement of [3H]TCP from rat brain NMDA receptor
12
Total Activities
12
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

New N-aryl-N'-(3-(substituted)phenyl)-N'-methylguanidines as leads to potential PET radioligands for imaging the open NMDA receptor.
Naumiec GR, Cai L, Pike VW.
Bioorg Med Chem Lett (2015) 25 : 225 -228
PubMed 25499436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.00 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356813 1 7.74
CHEMBL38936 1 7.50
CHEMBL3356812 1 7.43
CHEMBL3356798 1 7.40
CHEMBL3356809 1 7.27
CHEMBL3356829 1 7.11
CHEMBL3356800 1 6.96
CHEMBL3356817 1 6.82
CHEMBL3356815 1 6.35
CHEMBL3356803 1 6.27
CHEMBL3356826 1 6.15
CHEMBL3356799 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356813 Ki = 18.3 nM 7.74
CHEMBL38936 Ki = 31.9 nM 7.50
CHEMBL3356812 Ki = 36.7 nM 7.43
CHEMBL3356798 Ki = 39.8 nM 7.40
CHEMBL3356809 Ki = 53.7 nM 7.27
CHEMBL3356829 Ki = 78.4 nM 7.11
CHEMBL3356800 Ki = 110.0 nM 6.96
CHEMBL3356817 Ki = 152.0 nM 6.82
CHEMBL3356815 Ki = 447.0 nM 6.35
CHEMBL3356803 Ki = 540.0 nM 6.27
CHEMBL3356826 Ki = 701.0 nM 6.15
CHEMBL3356799 Ki > 1000.0 nM -