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Assay Detail

CHEMBL5383554

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

Binding
Displacement of [3H]ifenprodil from GluN2B in mouse LTK cells assessed as inhibition constant measured after 120 mins by scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type LTK
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL3442)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformationally Restricted σ<sub>1</sub> Receptor Antagonists from (-)-Isopulegol.
Blicker L, González-Cano R, Laurini E, Nieto FR, Schmidt J, Schepmann D, Pricl S, Wünsch B.
J Med Chem (2023) 66 : 4999 -5020
PubMed 36946301 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.88 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 9.22
CHEMBL493054 1 9.10
CHEMBL54 HALOPERIDOL 4.0 1 7.89
CHEMBL5415339 1 7.44
CHEMBL5435693 1 7.35
CHEMBL73824 1 7.31
CHEMBL5413704 1 7.28
CHEMBL5418583 1 7.21
CHEMBL5430693 1 7.04
CHEMBL5408176 1 6.90
CHEMBL5421431 1 6.69
CHEMBL5419171 1 6.58
CHEMBL5419345 1 6.57
CHEMBL5427418 1 6.50
CHEMBL5440135 1 6.44
CHEMBL5394456 1 6.43
CHEMBL5439989 1 6.39
CHEMBL5409031 1 6.37
CHEMBL5395928 1 6.29
CHEMBL5438476 1 6.29
CHEMBL5420805 1 6.05
CHEMBL5419756 1 5.97
CHEMBL5436332 1 5.89
CHEMBL5402137 1 5.89
CHEMBL2170062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 0.6 nM 9.22
CHEMBL493054 Ki = 0.8 nM 9.10
CHEMBL54 HALOPERIDOL Ki = 13.0 nM 7.89
CHEMBL5415339 Ki = 36.0 nM 7.44
CHEMBL5435693 Ki = 45.0 nM 7.35
CHEMBL73824 Ki = 49.0 nM 7.31
CHEMBL5413704 Ki = 53.0 nM 7.28
CHEMBL5418583 Ki = 61.0 nM 7.21
CHEMBL5430693 Ki = 92.0 nM 7.04
CHEMBL5408176 Ki = 125.0 nM 6.90
CHEMBL5421431 Ki = 205.0 nM 6.69
CHEMBL5419171 Ki = 263.0 nM 6.58
CHEMBL5419345 Ki = 267.0 nM 6.57
CHEMBL5427418 Ki = 313.0 nM 6.50
CHEMBL5440135 Ki = 363.0 nM 6.44
CHEMBL5394456 Ki = 370.0 nM 6.43
CHEMBL5439989 Ki = 408.0 nM 6.39
CHEMBL5409031 Ki = 423.0 nM 6.37
CHEMBL5395928 Ki = 511.0 nM 6.29
CHEMBL5438476 Ki = 508.0 nM 6.29
CHEMBL5420805 Ki = 890.0 nM 6.05
CHEMBL5419756 Ki = 1060.0 nM 5.97
CHEMBL5436332 Ki = 1300.0 nM 5.89
CHEMBL5402137 Ki = 1300.0 nM 5.89
CHEMBL2170062 Ki > 58.0 nM -