Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5732376

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

Binding
Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain homogenates. Twelve concentrations of each test ligand (0.001-1,000 nM) were incubated for 120 min at 25° C. in 50 mM Tris-HCl, pH 8.0 with 500 μg membrane protein, and 5 nM [3H](+)-pentazocine (for σ1 assays) or 3 nM [3H]DTG plus 300 nM (+)-pentazocine (for σ2 assays); non-specific binding was determined in the presence of 10 μM haloperidol. The assays were terminated with ice-cold 10 mM Tris-HCl, pH 8.0, followed by two washes through glass fiber filters that were pre-soaked for at least 30 min in 0.5% polyethyleneimine.
ChEMBL ↗
330
Total Activities
99
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Highly selective sigma receptor ligands and radioligands as probes in nociceptive processing and the pathphysiological study of memory deficits and cognitive disorders
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 110 7.73 9.51
kon 110 - -
k_off 110 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5847792 — — 3 9.51
CHEMBL5780878 — — 3 9.24
CHEMBL5964097 — — 3 9.03
CHEMBL272603 — — 3 8.89
CHEMBL6007417 — — 3 8.85
CHEMBL5759658 — — 3 8.70
CHEMBL6058223 — — 3 8.67
CHEMBL6039072 — — 3 8.66
CHEMBL5882203 — — 3 8.63
CHEMBL5762113 — — 3 8.62
CHEMBL5891701 — — 3 8.54
CHEMBL5874791 — — 3 8.50
CHEMBL5841076 — — 3 8.48
CHEMBL1830149 — — 3 8.48
CHEMBL408003 — — 3 8.47
CHEMBL6065416 — — 3 8.39
CHEMBL270341 — — 6 8.38
CHEMBL5741168 — — 3 8.35
CHEMBL272610 — — 6 8.34
CHEMBL5954856 — — 3 8.33
CHEMBL271975 — — 6 8.33
CHEMBL272854 — — 3 8.31
CHEMBL406081 — — 6 8.30
CHEMBL5926988 — — 3 8.30
CHEMBL405925 — — 6 8.28
CHEMBL273084 — — 6 8.25
CHEMBL5871856 — — 3 8.23
CHEMBL6015330 — — 3 8.21
CHEMBL5833294 — — 3 8.20
CHEMBL272608 — — 6 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5847792 — Ki = 0.31 nM 9.51
CHEMBL5780878 — Ki = 0.58 nM 9.24
CHEMBL5964097 — Ki = 0.94 nM 9.03
CHEMBL272603 — Ki = 1.28 nM 8.89
CHEMBL6007417 — Ki = 1.43 nM 8.85
CHEMBL5759658 — Ki = 2.01 nM 8.70
CHEMBL6058223 — Ki = 2.15 nM 8.67
CHEMBL6039072 — Ki = 2.18 nM 8.66
CHEMBL5882203 — Ki = 2.36 nM 8.63
CHEMBL5762113 — Ki = 2.4 nM 8.62
CHEMBL5891701 — Ki = 2.89 nM 8.54
CHEMBL5874791 — Ki = 3.15 nM 8.50
CHEMBL5841076 — Ki = 3.33 nM 8.48
CHEMBL1830149 — Ki = 3.28 nM 8.48
CHEMBL408003 — Ki = 3.37 nM 8.47
CHEMBL6065416 — Ki = 4.04 nM 8.39
CHEMBL270341 — Ki = 4.17 nM 8.38
CHEMBL270341 — Ki = 4.17 nM 8.38
CHEMBL5741168 — Ki = 4.44 nM 8.35
CHEMBL272610 — Ki = 4.6 nM 8.34
CHEMBL272610 — Ki = 4.6 nM 8.34
CHEMBL271975 — Ki = 4.66 nM 8.33
CHEMBL271975 — Ki = 4.66 nM 8.33
CHEMBL5954856 — Ki = 4.68 nM 8.33
CHEMBL272854 — Ki = 4.9 nM 8.31
CHEMBL406081 — Ki = 4.98 nM 8.30
CHEMBL5926988 — Ki = 5.04 nM 8.30
CHEMBL406081 — Ki = 4.98 nM 8.30
CHEMBL405925 — Ki = 5.22 nM 8.28
CHEMBL405925 — Ki = 5.22 nM 8.28
CHEMBL273084 — Ki = 5.61 nM 8.25
CHEMBL273084 — Ki = 5.61 nM 8.25
CHEMBL5871856 — Ki = 5.94 nM 8.23
CHEMBL6015330 — Ki = 6.24 nM 8.21
CHEMBL5833294 — Ki = 6.27 nM 8.20
CHEMBL272608 — Ki = 6.55 nM 8.18
CHEMBL272608 — Ki = 6.55 nM 8.18
CHEMBL6043522 — Ki = 6.75 nM 8.17
CHEMBL269876 — Ki = 6.9 nM 8.16
CHEMBL269876 — Ki = 6.9 nM 8.16
CHEMBL5995507 — Ki = 7.21 nM 8.14
CHEMBL6039012 — Ki = 7.42 nM 8.13
CHEMBL5898109 — Ki = 7.59 nM 8.12
CHEMBL6051457 — Ki = 7.5 nM 8.12
CHEMBL6016109 — Ki = 7.87 nM 8.10
CHEMBL5860120 — Ki = 8.73 nM 8.06
CHEMBL6004354 — Ki = 8.94 nM 8.05
CHEMBL5803138 — Ki = 9.11 nM 8.04
CHEMBL6063068 — Ki = 10.8 nM 7.97
CHEMBL406082 — Ki = 10.6 nM 7.97