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Assay Detail

CHEMBL5732377

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
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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 8.02 10.26
kon 110 - -
k_off 110 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5871856 — — 3 10.26
CHEMBL1831157 — — 3 9.68
CHEMBL5759658 — — 3 9.66
CHEMBL270341 — — 6 9.41
CHEMBL4584941 — — 3 9.34
CHEMBL5995507 — — 3 9.30
CHEMBL272603 — — 3 9.26
CHEMBL5803138 — — 3 9.25
CHEMBL5891701 — — 3 9.18
CHEMBL5898109 — — 3 9.15
CHEMBL272854 — — 3 9.11
CHEMBL6004354 — — 3 9.00
CHEMBL1831156 — — 3 8.96
CHEMBL5956269 — — 3 8.92
CHEMBL272608 — — 6 8.83
CHEMBL6018499 — — 3 8.82
CHEMBL5789726 — — 3 8.78
CHEMBL5847792 — — 3 8.75
CHEMBL271772 — — 6 8.74
CHEMBL6063068 — — 3 8.73
CHEMBL1830149 — — 3 8.72
CHEMBL6055931 — — 3 8.71
CHEMBL5926988 — — 3 8.67
CHEMBL5980797 — — 3 8.67
CHEMBL271975 — — 6 8.65
CHEMBL5751077 — — 3 8.61
CHEMBL6058223 — — 3 8.61
CHEMBL406081 — — 6 8.61
CHEMBL6039072 — — 3 8.59
CHEMBL4563981 — — 3 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5871856 — Ki = 0.055 nM 10.26
CHEMBL1831157 — Ki = 0.21 nM 9.68
CHEMBL5759658 — Ki = 0.22 nM 9.66
CHEMBL270341 — Ki = 0.39 nM 9.41
CHEMBL270341 — Ki = 0.39 nM 9.41
CHEMBL4584941 — Ki = 0.46 nM 9.34
CHEMBL5995507 — Ki = 0.5 nM 9.30
CHEMBL272603 — Ki = 0.55 nM 9.26
CHEMBL5803138 — Ki = 0.56 nM 9.25
CHEMBL5891701 — Ki = 0.66 nM 9.18
CHEMBL5898109 — Ki = 0.7 nM 9.15
CHEMBL272854 — Ki = 0.77 nM 9.11
CHEMBL6004354 — Ki = 0.99 nM 9.00
CHEMBL1831156 — Ki = 1.09 nM 8.96
CHEMBL5956269 — Ki = 1.21 nM 8.92
CHEMBL272608 — Ki = 1.49 nM 8.83
CHEMBL272608 — Ki = 1.49 nM 8.83
CHEMBL6018499 — Ki = 1.52 nM 8.82
CHEMBL5789726 — Ki = 1.67 nM 8.78
CHEMBL5847792 — Ki = 1.76 nM 8.75
CHEMBL271772 — Ki = 1.83 nM 8.74
CHEMBL271772 — Ki = 1.83 nM 8.74
CHEMBL6063068 — Ki = 1.88 nM 8.73
CHEMBL1830149 — Ki = 1.9 nM 8.72
CHEMBL6055931 — Ki = 1.96 nM 8.71
CHEMBL5926988 — Ki = 2.12 nM 8.67
CHEMBL5980797 — Ki = 2.15 nM 8.67
CHEMBL271975 — Ki = 2.25 nM 8.65
CHEMBL271975 — Ki = 2.25 nM 8.65
CHEMBL406081 — Ki = 2.44 nM 8.61
CHEMBL5751077 — Ki = 2.46 nM 8.61
CHEMBL6058223 — Ki = 2.43 nM 8.61
CHEMBL406081 — Ki = 2.44 nM 8.61
CHEMBL6039072 — Ki = 2.56 nM 8.59
CHEMBL4563981 — Ki = 2.57 nM 8.59
CHEMBL6021878 — Ki = 2.79 nM 8.55
CHEMBL273084 — Ki = 3.05 nM 8.52
CHEMBL273084 — Ki = 3.05 nM 8.52
CHEMBL272610 — Ki = 3.06 nM 8.51
CHEMBL272610 — Ki = 3.06 nM 8.51
CHEMBL5860120 — Ki = 3.15 nM 8.50
CHEMBL5761676 — Ki = 3.59 nM 8.45
CHEMBL6043522 — Ki = 3.73 nM 8.43
CHEMBL408003 — Ki = 3.77 nM 8.42
CHEMBL6051457 — Ki = 4.02 nM 8.40
CHEMBL1831166 — Ki = 4.37 nM 8.36
CHEMBL6016109 — Ki = 4.47 nM 8.35
CHEMBL5827818 — Ki = 4.72 nM 8.33
CHEMBL5913929 — Ki = 4.85 nM 8.31
CHEMBL269876 — Ki = 5.43 nM 8.27