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Assay Detail

CHEMBL5365001

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

Binding
Displacement of [3H]ifenprodil from human GluN2B expressed in mouse L-M(TK-) cell membrane coexpressing GluN1a assessed as inhibition constant measured after 120 mins by competitive binding assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type L-M(TK-)
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
Lüken J, Goerges G, Ritter N, Disse P, Schreiber JA, Schmidt J, Frehland B, Schepmann D, Seebohm G, Wünsch B.
J Med Chem (2023) 66 : 11573 -11588
PubMed 37580890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.52 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410173 1 8.24
CHEMBL305187 IFENPRODIL 2.0 1 8.24
CHEMBL5421604 1 8.18
CHEMBL114644 1 7.96
CHEMBL5441115 1 7.92
CHEMBL5435194 1 7.89
CHEMBL5432456 1 7.89
CHEMBL5398972 1 7.75
CHEMBL5423529 1 7.70
CHEMBL5406518 1 7.70
CHEMBL5409908 1 7.60
CHEMBL5396018 1 7.54
CHEMBL5410339 1 7.50
CHEMBL5429038 1 7.46
CHEMBL5432037 1 7.42
CHEMBL5416753 1 7.42
CHEMBL5425955 1 7.42
CHEMBL5408501 1 7.38
CHEMBL5435626 1 7.28
CHEMBL5431988 1 7.25
CHEMBL5417143 1 7.03
CHEMBL5440346 1 6.92
CHEMBL5403196 1 6.87
CHEMBL5394862 1 6.74
CHEMBL5435354 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410173 Ki = 5.7 nM 8.24
CHEMBL305187 IFENPRODIL Ki = 5.8 nM 8.24
CHEMBL5421604 Ki = 6.6 nM 8.18
CHEMBL114644 Ki = 11.0 nM 7.96
CHEMBL5441115 Ki = 12.0 nM 7.92
CHEMBL5435194 Ki = 13.0 nM 7.89
CHEMBL5432456 Ki = 13.0 nM 7.89
CHEMBL5398972 Ki = 18.0 nM 7.75
CHEMBL5423529 Ki = 20.0 nM 7.70
CHEMBL5406518 Ki = 20.0 nM 7.70
CHEMBL5409908 Ki = 25.0 nM 7.60
CHEMBL5396018 Ki = 29.0 nM 7.54
CHEMBL5410339 Ki = 32.0 nM 7.50
CHEMBL5429038 Ki = 35.0 nM 7.46
CHEMBL5432037 Ki = 38.0 nM 7.42
CHEMBL5416753 Ki = 38.0 nM 7.42
CHEMBL5425955 Ki = 38.0 nM 7.42
CHEMBL5408501 Ki = 42.0 nM 7.38
CHEMBL5435626 Ki = 53.0 nM 7.28
CHEMBL5431988 Ki = 56.0 nM 7.25
CHEMBL5417143 Ki = 93.0 nM 7.03
CHEMBL5440346 Ki = 120.0 nM 6.92
CHEMBL5403196 Ki = 136.0 nM 6.87
CHEMBL5394862 Ki = 182.0 nM 6.74
CHEMBL5435354 Ki = 265.0 nM 6.58