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Assay Detail

CHEMBL1930738

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

Binding
Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities as σ₁ receptor ligands.
Ferorelli S, Abate C, Pedone MP, Colabufo NA, Contino M, Perrone R, Berardi F.
Bioorg Med Chem (2011) 19 : 7612 -7622
PubMed 22075234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.81 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1929287 1 7.71
CHEMBL1929280 1 7.55
CHEMBL282433 DITOLYLGUANIDINE 1 7.46
CHEMBL1929281 1 7.43
CHEMBL1929279 1 7.42
CHEMBL1929277 1 7.37
CHEMBL1929278 1 7.20
CHEMBL1929282 1 7.18
CHEMBL1929286 1 6.96
CHEMBL1929276 1 6.92
CHEMBL1929284 1 6.71
CHEMBL1929275 1 6.62
CHEMBL128358 1 6.61
CHEMBL1929430 1 6.38
CHEMBL1929428 1 6.13
CHEMBL1929283 1 5.74
CHEMBL1929285 1 5.70
CHEMBL1929429 1 5.48
CHEMBL1929288 1 -
CHEMBL1929289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1929287 Ki = 19.6 nM 7.71
CHEMBL1929280 Ki = 28.1 nM 7.55
CHEMBL282433 DITOLYLGUANIDINE Ki = 34.3 nM 7.46
CHEMBL1929281 Ki = 37.5 nM 7.43
CHEMBL1929279 Ki = 38.0 nM 7.42
CHEMBL1929277 Ki = 42.3 nM 7.37
CHEMBL1929278 Ki = 63.6 nM 7.20
CHEMBL1929282 Ki = 65.9 nM 7.18
CHEMBL1929286 Ki = 110.0 nM 6.96
CHEMBL1929276 Ki = 119.0 nM 6.92
CHEMBL1929284 Ki = 194.0 nM 6.71
CHEMBL1929275 Ki = 242.0 nM 6.62
CHEMBL128358 Ki = 247.0 nM 6.61
CHEMBL1929430 Ki = 414.0 nM 6.38
CHEMBL1929428 Ki = 742.0 nM 6.13
CHEMBL1929283 Ki = 1810.0 nM 5.74
CHEMBL1929285 Ki = 1990.0 nM 5.70
CHEMBL1929429 Ki = 3330.0 nM 5.48
CHEMBL1929288 Ki > 10000.0 nM -
CHEMBL1929289 Ki > 10000.0 nM -