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Assay Detail

CHEMBL1930739

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

Binding
Displacement of [3H]-emopamil from delta(8)-delta(7) sterol isomerase in guinea pig liver membranes
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (CHEMBL5525)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 15 8.21 9.70
Ki(app) 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1929281 1 9.70
CHEMBL128358 1 9.17
CHEMBL1929278 1 9.05
CHEMBL1929277 1 8.96
CHEMBL1929275 1 8.81
CHEMBL1929280 1 8.68
CHEMBL1929279 1 8.51
CHEMBL1929287 1 8.42
CHEMBL1929282 1 8.14
CHEMBL305187 IFENPRODIL 2.0 1 7.82
CHEMBL1929428 1 6.94
CHEMBL1929430 1 6.67
CHEMBL1929429 1 5.85
CHEMBL1929284 1 -
CHEMBL1929285 1 -
CHEMBL1929286 1 -
CHEMBL1929283 1 -
CHEMBL1929288 1 -
CHEMBL1929289 1 -
CHEMBL1929276 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1929281 Ki = 0.2 nM 9.70
CHEMBL128358 Ki = 0.67 nM 9.17
CHEMBL1929278 Ki = 0.9 nM 9.05
CHEMBL1929277 Ki = 1.1 nM 8.96
CHEMBL1929275 Ki = 1.54 nM 8.81
CHEMBL1929280 Ki = 2.11 nM 8.68
CHEMBL1929279 Ki = 3.07 nM 8.51
CHEMBL1929287 Ki = 3.8 nM 8.42
CHEMBL1929282 Ki = 7.3 nM 8.14
CHEMBL305187 IFENPRODIL Ki = 15.0 nM 7.82
CHEMBL1929428 Ki = 115.0 nM 6.94
CHEMBL1929430 Ki = 213.0 nM 6.67
CHEMBL1929429 Ki = 1400.0 nM 5.85
CHEMBL1929284 Ki(app) - -
CHEMBL1929285 Ki(app) - -
CHEMBL1929286 Ki(app) - -
CHEMBL1929283 Ki(app) - -
CHEMBL1929288 Ki > 10000.0 nM -
CHEMBL1929289 Ki > 10000.0 nM -
CHEMBL1929276 Ki(app) - -