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Assay Detail

CHEMBL3737381

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 membranes by scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.49 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735947 1 7.96
CHEMBL3736502 1 7.96
CHEMBL3735173 1 7.80
CHEMBL3735485 1 7.36
CHEMBL282433 DITOLYLGUANIDINE 1 7.24
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL319706 (S)-IFENPRODIL 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735947 Ki = 11.0 nM 7.96
CHEMBL3736502 Ki = 11.0 nM 7.96
CHEMBL3735173 Ki = 16.0 nM 7.80
CHEMBL3735485 Ki = 44.0 nM 7.36
CHEMBL282433 DITOLYLGUANIDINE Ki = 57.0 nM 7.24
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL319706 (S)-IFENPRODIL Ki = 98.0 nM 7.01