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Assay Detail

CHEMBL1000138

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

Binding
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cortical membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 5.89 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140287 1 6.29
CHEMBL138900 1 6.23
CHEMBL485729 1 6.15
CHEMBL521350 1 6.11
CHEMBL485929 1 6.11
CHEMBL485728 1 5.65
CHEMBL139848 1 5.29
CHEMBL487360 1 5.26
CHEMBL487359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140287 Ki = 512.0 nM 6.29
CHEMBL138900 Ki = 585.0 nM 6.23
CHEMBL485729 Ki = 712.0 nM 6.15
CHEMBL521350 Ki = 783.0 nM 6.11
CHEMBL485929 Ki = 786.0 nM 6.11
CHEMBL485728 Ki = 2250.0 nM 5.65
CHEMBL139848 Ki = 5160.0 nM 5.29
CHEMBL487360 Ki = 5540.0 nM 5.26
CHEMBL487359 Ki > 850.0 nM -