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Assay Detail

CHEMBL1000139

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

Binding
Displacement of [3H](-)-(S)-emopamil from EBP in guinea pig liver membrane
30
Total Activities
30
Compounds Tested
1
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

Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.
Berardi F, Abate C, Ferorelli S, de Robertis AF, Leopoldo M, Colabufo NA, Niso M, Perrone R.
J Med Chem (2008) 51 : 7523 -7531
PubMed 19053780 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.35 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457722 1 8.30
CHEMBL456435 1 8.30
CHEMBL513936 1 8.15
CHEMBL457720 1 8.14
CHEMBL485729 1 8.09
CHEMBL53325 1 8.08
CHEMBL457508 1 8.04
CHEMBL486136 1 7.87
CHEMBL190883 1 7.84
CHEMBL305187 IFENPRODIL 2.0 1 7.79
CHEMBL511857 1 7.79
CHEMBL487360 1 7.78
CHEMBL456437 1 7.78
CHEMBL487359 1 7.63
CHEMBL138900 1 7.49
CHEMBL511680 1 7.48
CHEMBL485929 1 7.48
CHEMBL521350 1 7.34
CHEMBL457731 1 7.33
CHEMBL458553 1 7.31
CHEMBL458361 1 7.14
CHEMBL458802 1 7.07
CHEMBL457721 1 6.97
CHEMBL511507 1 6.85
CHEMBL139848 1 6.34
CHEMBL75228 1-PHENETHYLPIPERIDINE 1 6.22
CHEMBL485728 1 5.77
CHEMBL140287 1 5.58
CHEMBL282433 DITOLYLGUANIDINE 1 5.12
CHEMBL60542 (+)-PENTAZOCINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457722 Ki = 4.95 nM 8.30
CHEMBL456435 Ki = 5.0 nM 8.30
CHEMBL513936 Ki = 7.0 nM 8.15
CHEMBL457720 Ki = 7.21 nM 8.14
CHEMBL485729 Ki = 8.15 nM 8.09
CHEMBL53325 Ki = 8.38 nM 8.08
CHEMBL457508 Ki = 9.04 nM 8.04
CHEMBL486136 Ki = 13.5 nM 7.87
CHEMBL190883 Ki = 14.6 nM 7.84
CHEMBL305187 IFENPRODIL Ki = 16.4 nM 7.79
CHEMBL511857 Ki = 16.2 nM 7.79
CHEMBL487360 Ki = 16.7 nM 7.78
CHEMBL456437 Ki = 16.8 nM 7.78
CHEMBL487359 Ki = 23.5 nM 7.63
CHEMBL138900 Ki = 32.1 nM 7.49
CHEMBL511680 Ki = 33.1 nM 7.48
CHEMBL485929 Ki = 32.8 nM 7.48
CHEMBL521350 Ki = 45.4 nM 7.34
CHEMBL457731 Ki = 46.7 nM 7.33
CHEMBL458553 Ki = 49.2 nM 7.31
CHEMBL458361 Ki = 71.6 nM 7.14
CHEMBL458802 Ki = 85.1 nM 7.07
CHEMBL457721 Ki = 106.0 nM 6.97
CHEMBL511507 Ki = 140.0 nM 6.85
CHEMBL139848 Ki = 460.0 nM 6.34
CHEMBL75228 1-PHENETHYLPIPERIDINE Ki = 595.0 nM 6.22
CHEMBL485728 Ki = 1710.0 nM 5.77
CHEMBL140287 Ki = 2640.0 nM 5.58
CHEMBL282433 DITOLYLGUANIDINE Ki = 7660.0 nM 5.12
CHEMBL60542 (+)-PENTAZOCINE Ki > 10.0 nM -