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Assay Detail

CHEMBL1000142

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Functional
Antiproliferative activity against human PC3 cells expressing EBP after 48 hrs by MTT assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Autocuration

Target

PC-3 (CHEMBL390)
Type CELL-LINE
Organism Homo sapiens

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 9 7.50 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457722 1 7.89
CHEMBL485729 1 7.71
CHEMBL511857 1 7.64
CHEMBL305187 IFENPRODIL 2.0 1 7.59
CHEMBL511507 1 7.43
CHEMBL456435 1 7.42
CHEMBL53325 1 7.42
CHEMBL190883 1 7.33
CHEMBL60542 (+)-PENTAZOCINE 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457722 Ki = 12.9 nM 7.89
CHEMBL485729 Ki = 19.3 nM 7.71
CHEMBL511857 Ki = 23.0 nM 7.64
CHEMBL305187 IFENPRODIL Ki = 25.8 nM 7.59
CHEMBL511507 Ki = 37.3 nM 7.43
CHEMBL456435 Ki = 38.0 nM 7.42
CHEMBL53325 Ki = 37.7 nM 7.42
CHEMBL190883 Ki = 47.0 nM 7.33
CHEMBL60542 (+)-PENTAZOCINE Ki = 86.9 nM 7.06