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Assay Detail

CHEMBL4615566

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

Binding
Displacement of [3H]ifenprodil from GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method
10
Total Activities
10
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

Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
Zampieri D, Fortuna S, Calabretti A, Romano M, Menegazzi R, Schepmann D, Wünsch B, Mamolo MG.
ACS Med Chem Lett (2020) 11 : 651 -656
PubMed 32435366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.80 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305187 IFENPRODIL 2.0 1 8.00
CHEMBL4643805 1 7.23
CHEMBL4644807 1 7.10
CHEMBL4640137 1 6.97
CHEMBL4643145 1 6.94
CHEMBL4636728 1 6.53
CHEMBL4633788 1 5.82
CHEMBL4639180 1 5.80
CHEMBL54 HALOPERIDOL 4.0 1 -
CHEMBL282433 DITOLYLGUANIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305187 IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL4643805 Ki = 59.0 nM 7.23
CHEMBL4644807 Ki = 79.0 nM 7.10
CHEMBL4640137 Ki = 108.0 nM 6.97
CHEMBL4643145 Ki = 116.0 nM 6.94
CHEMBL4636728 Ki = 294.0 nM 6.53
CHEMBL4633788 Ki = 1500.0 nM 5.82
CHEMBL4639180 Ki = 1600.0 nM 5.80
CHEMBL54 HALOPERIDOL Ki - -
CHEMBL282433 DITOLYLGUANIDINE Ki - -