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Assay Detail

CHEMBL752263

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

Binding
Inhibition of [3H]25-6981 binding to N-methyl-D-aspartate glutamate receptor 2B of rat brain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.
Bioorg Med Chem Lett (2003) 13 : 1759 -1762
PubMed 12729659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.30 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299294 1 8.70
CHEMBL50872 1 8.46
CHEMBL51594 1 8.10
CHEMBL48915 1 8.10
CHEMBL49623 (R,S)-IFENPRODIL 1 7.89
CHEMBL46779 1 7.60
CHEMBL48366 1 7.58
CHEMBL50166 1 7.54
CHEMBL48743 1 7.43
CHEMBL294961 1 7.12
CHEMBL433092 1 6.64
CHEMBL46251 1 5.25
CHEMBL48365 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299294 Ki = 2.0 nM 8.70
CHEMBL50872 Ki = 3.5 nM 8.46
CHEMBL51594 Ki = 8.0 nM 8.10
CHEMBL48915 Ki = 8.0 nM 8.10
CHEMBL49623 (R,S)-IFENPRODIL Ki = 13.0 nM 7.89
CHEMBL46779 Ki = 25.0 nM 7.60
CHEMBL48366 Ki = 26.0 nM 7.58
CHEMBL50166 Ki = 29.0 nM 7.54
CHEMBL48743 Ki = 37.0 nM 7.43
CHEMBL294961 Ki = 75.0 nM 7.12
CHEMBL433092 Ki = 230.0 nM 6.64
CHEMBL46251 Ki = 5600.0 nM 5.25
CHEMBL48365 Ki = 28000.0 nM 4.55