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Assay Detail

CHEMBL833650

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Functional
Binding affinity for alpha-2A-adrenergic receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Fernández J, Font LM, Hens KA, Iturrino L, Lenaerts I, Martínez S, Megens AA, Pastor J, Vermote PC, Steckler T.
J Med Chem (2005) 48 : 2054 -2071
PubMed 15771448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.75 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91157 1 9.10
CHEMBL419316 1 8.85
CHEMBL92860 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91157 Ki = 0.8 nM 9.10
CHEMBL419316 Ki = 1.4 nM 8.85
CHEMBL92860 Ki = 5.0 nM 8.30