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Assay Detail

CHEMBL2156104

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

Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-adrenergic receptor blocking properties.
Romeiro LA, da Silva Ferreira M, da Silva LL, Castro HC, Miranda AL, Silva CL, Noël F, Nascimento JB, Araújo CV, Tibiriçá E, Barreiro EJ, Fraga CA.
Eur J Med Chem (2011) 46 : 3000 -3012
PubMed 21549456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.87 9.89
IC50 1 9.57 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 9.89
CHEMBL2153423 2 9.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Ki = 0.13 nM 9.89
CHEMBL2153423 Ki = 0.14 nM 9.85
CHEMBL2153423 IC50 = 0.2692 nM 9.57