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Assay Detail

CHEMBL4307196

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

Binding
Displacement of [3H]ifenprodil from GluN1a/GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes after 120 mins by solid scintillation counting method
17
Total Activities
17
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

Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
Zampieri D, Fortuna S, Calabretti A, Romano M, Menegazzi R, Schepmann D, Wünsch B, Collina S, Zanon D, Mamolo MG.
Eur J Med Chem (2019) 180 : 268 -282
PubMed 31319263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.65 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581662 1 8.70
CHEMBL4533030 1 8.30
CHEMBL4459690 1 8.30
CHEMBL4446466 1 8.09
CHEMBL4449269 1 8.09
CHEMBL4445874 1 8.00
CHEMBL4439170 1 7.92
CHEMBL4451677 1 7.64
CHEMBL4446431 1 7.58
CHEMBL4446009 1 7.57
CHEMBL4463741 1 7.24
CHEMBL4567801 1 7.17
CHEMBL4453315 1 7.11
CHEMBL4442750 1 6.65
CHEMBL4454333 1 6.38
CHEMBL54 HALOPERIDOL 4.0 1 -
CHEMBL282433 DITOLYLGUANIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581662 Ki = 2.0 nM 8.70
CHEMBL4533030 Ki = 5.0 nM 8.30
CHEMBL4459690 Ki = 5.0 nM 8.30
CHEMBL4446466 Ki = 8.2 nM 8.09
CHEMBL4449269 Ki = 8.1 nM 8.09
CHEMBL4445874 Ki = 10.0 nM 8.00
CHEMBL4439170 Ki = 12.0 nM 7.92
CHEMBL4451677 Ki = 23.0 nM 7.64
CHEMBL4446431 Ki = 26.0 nM 7.58
CHEMBL4446009 Ki = 27.0 nM 7.57
CHEMBL4463741 Ki = 58.0 nM 7.24
CHEMBL4567801 Ki = 68.0 nM 7.17
CHEMBL4453315 Ki = 78.0 nM 7.11
CHEMBL4442750 Ki = 226.0 nM 6.65
CHEMBL4454333 Ki = 412.0 nM 6.38
CHEMBL54 HALOPERIDOL Ki - -
CHEMBL282433 DITOLYLGUANIDINE Ki - -