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Assay Detail

CHEMBL804438

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

Binding
Inhibition of [3H]-emopamil binding to Sterol delta 8-delta 7 isomerase in guinea pig liver membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
Berardi F, Loiodice F, Fracchiolla G, Colabufo NA, Perrone R, Tortorella V.
J Med Chem (2003) 46 : 2117 -2124
PubMed 12747784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.96 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305187 IFENPRODIL 2.0 1 8.57
CHEMBL542392 1 8.47
CHEMBL555790 1 8.43
CHEMBL543821 1 8.43
CHEMBL545691 1 8.11
CHEMBL540289 1 8.02
CHEMBL543581 1 7.92
CHEMBL539776 1 7.84
CHEMBL543105 1 7.73
CHEMBL542873 1 7.56
CHEMBL555090 1 7.52
CHEMBL545451 1 7.46
CHEMBL544524 1 7.43
CHEMBL544992 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305187 IFENPRODIL Ki = 2.71 nM 8.57
CHEMBL542392 Ki = 3.38 nM 8.47
CHEMBL555790 Ki = 3.73 nM 8.43
CHEMBL543821 Ki = 3.7 nM 8.43
CHEMBL545691 Ki = 7.79 nM 8.11
CHEMBL540289 Ki = 9.65 nM 8.02
CHEMBL543581 Ki = 12.0 nM 7.92
CHEMBL539776 Ki = 14.5 nM 7.84
CHEMBL543105 Ki = 18.7 nM 7.73
CHEMBL542873 Ki = 27.5 nM 7.56
CHEMBL555090 Ki = 30.1 nM 7.52
CHEMBL545451 Ki = 35.1 nM 7.46
CHEMBL544524 Ki = 37.0 nM 7.43
CHEMBL544992 Ki > - nM -