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Assay Detail

CHEMBL3757723

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

Binding
Displacement of [3H]ifenprodil from recombinant human GluN1a/GluN2B expressed in L(tk-)cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
Dey S, Schepmann D, Wünsch B.
Bioorg Med Chem Lett (2016) 26 : 889 -893
PubMed 26750254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.09 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319706 (S)-IFENPRODIL 1 8.00
CHEMBL1289626 1 7.85
CHEMBL3753409 1 7.14
CHEMBL3752293 1 6.39
CHEMBL3752701 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319706 (S)-IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL1289626 Ki = 14.0 nM 7.85
CHEMBL3753409 Ki = 73.0 nM 7.14
CHEMBL3752293 Ki = 404.0 nM 6.39
CHEMBL3752701 Ki = 887.0 nM 6.05