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Assay Detail

CHEMBL4349901

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(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
Wagner M, Schepmann D, Ametamey SM, Wünsch B.
Bioorg Med Chem (2019) 27 : 3559 -3567
PubMed 31255496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.02 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113830 (S,R)-IFENPRODIL 1 8.00
CHEMBL28564 ELIPRODIL 2.0 1 7.89
CHEMBL4439555 1 6.71
CHEMBL4472450 1 6.34
CHEMBL1289403 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113830 (S,R)-IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL28564 ELIPRODIL Ki = 13.0 nM 7.89
CHEMBL4439555 Ki = 193.0 nM 6.71
CHEMBL4472450 Ki = 460.0 nM 6.34
CHEMBL1289403 Ki = 706.0 nM 6.15