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Assay Detail

CHEMBL1000137

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

Binding
Displacement of [3H]spiroperidol from dopamine D2 receptor in rat striatal membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 5.85 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487359 1 6.11
CHEMBL485929 1 6.10
CHEMBL140287 1 5.91
CHEMBL487360 1 5.88
CHEMBL485729 1 5.67
CHEMBL139848 1 5.66
CHEMBL485728 1 5.62
CHEMBL138900 1 -
CHEMBL521350 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487359 Ki = 783.0 nM 6.11
CHEMBL485929 Ki = 787.0 nM 6.10
CHEMBL140287 Ki = 1220.0 nM 5.91
CHEMBL487360 Ki = 1310.0 nM 5.88
CHEMBL485729 Ki = 2120.0 nM 5.67
CHEMBL139848 Ki = 2190.0 nM 5.66
CHEMBL485728 Ki = 2380.0 nM 5.62
CHEMBL138900 Ki > 850.0 nM -
CHEMBL521350 Ki > 850.0 nM -