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Assay Detail

CHEMBL3300409

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

Binding
Displacement of (+)-DTG from sigma2 receptor in rat liver membrane by scintillation counting analysis
23
Total Activities
23
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

Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands.
Laurini E, Harel D, Marson D, Schepmann D, Schmidt TJ, Pricl S, Wünsch B.
Eur J Med Chem (2014) 83 : 526 -533
PubMed 24996139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.26 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.24
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL2435435 1 6.89
CHEMBL2435442 1 6.88
CHEMBL2435425 1 6.82
CHEMBL2435428 1 6.81
CHEMBL2435427 1 6.65
CHEMBL2435441 1 6.54
CHEMBL2435431 1 6.46
CHEMBL3298974 1 6.46
CHEMBL2435437 1 6.42
CHEMBL2435438 1 6.27
CHEMBL2435426 1 6.07
CHEMBL2435443 1 6.01
CHEMBL2435433 1 5.97
CHEMBL3298973 1 5.90
CHEMBL2435440 1 5.85
CHEMBL3298885 1 5.80
CHEMBL2435434 1 5.77
CHEMBL2435439 1 5.66
CHEMBL2435424 1 5.64
CHEMBL2435429 1 5.62
CHEMBL2435430 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 57.0 nM 7.24
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL2435435 Ki = 128.0 nM 6.89
CHEMBL2435442 Ki = 133.0 nM 6.88
CHEMBL2435425 Ki = 152.0 nM 6.82
CHEMBL2435428 Ki = 156.0 nM 6.81
CHEMBL2435427 Ki = 226.0 nM 6.65
CHEMBL2435441 Ki = 292.0 nM 6.54
CHEMBL2435431 Ki = 348.0 nM 6.46
CHEMBL3298974 Ki = 343.0 nM 6.46
CHEMBL2435437 Ki = 378.0 nM 6.42
CHEMBL2435438 Ki = 540.0 nM 6.27
CHEMBL2435426 Ki = 850.0 nM 6.07
CHEMBL2435443 Ki = 972.0 nM 6.01
CHEMBL2435433 Ki = 1080.0 nM 5.97
CHEMBL3298973 Ki = 1250.0 nM 5.90
CHEMBL2435440 Ki = 1400.0 nM 5.85
CHEMBL3298885 Ki = 1600.0 nM 5.80
CHEMBL2435434 Ki = 1700.0 nM 5.77
CHEMBL2435439 Ki = 2180.0 nM 5.66
CHEMBL2435424 Ki = 2290.0 nM 5.64
CHEMBL2435429 Ki = 2380.0 nM 5.62
CHEMBL2435430 Ki = 9260.0 nM 5.03