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Assay Detail

CHEMBL3801686

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

Binding
Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate incubated for 120 mins by solid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
Lütnant I, Schepmann D, Wünsch B.
Eur J Med Chem (2016) 116 : 136 -146
PubMed 27061977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.91 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.24
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL319706 (S)-IFENPRODIL 1 7.01
CHEMBL3797704 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 57.5 nM 7.24
CHEMBL54 HALOPERIDOL Ki = 78.1 nM 7.11
CHEMBL319706 (S)-IFENPRODIL Ki = 98.3 nM 7.01
CHEMBL3797704 Ki = 549.0 nM 6.26