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Assay Detail

CHEMBL3737377

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

Binding
Displacement of [3H]ifenprodil from Glun2B receptor (unknown origin) expressed in mouse L(tk-) cell membranes after 120 mins by scintillation counting analysis
7
Total Activities
7
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

Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.
Gawaskar S, Schepmann D, Bonifazi A, Robaa D, Sippl W, Wünsch B.
Bioorg Med Chem Lett (2015) 25 : 5748 -5751
PubMed 26531150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.24 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735947 1 8.80
CHEMBL3735485 1 8.48
CHEMBL3736502 1 8.42
CHEMBL3735173 1 8.12
CHEMBL319706 (S)-IFENPRODIL 1 8.00
CHEMBL3357784 1 8.00
CHEMBL28564 ELIPRODIL 2.0 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735947 Ki = 1.6 nM 8.80
CHEMBL3735485 Ki = 3.3 nM 8.48
CHEMBL3736502 Ki = 3.8 nM 8.42
CHEMBL3735173 Ki = 7.6 nM 8.12
CHEMBL319706 (S)-IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL3357784 Ki = 10.0 nM 8.00
CHEMBL28564 ELIPRODIL Ki = 13.0 nM 7.89