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Assay Detail

CHEMBL905524

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

Binding
Displacement of [3H]rawolscine from human cloned adrenergic Alpha-2C receptor transfected in CHO cells
9
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-2C adrenergic receptor (CHEMBL1916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Drinkenburg W, Fernández J, Font LM, Iturrino L, Langlois X, Lenaerts I, Martínez S, Megens AA, Pastor J, Pullan S, Steckler T.
Bioorg Med Chem (2007) 15 : 3649 -3660
PubMed 17407815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.55 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390718 3 10.00
CHEMBL318235 3 9.57
CHEMBL226636 3 8.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390718 Ki = 0.1 nM 10.00
CHEMBL318235 Ki = 0.27 nM 9.57
CHEMBL318235 Ki = 0.7 nM 9.15
CHEMBL390718 Ki = 0.93 nM 9.03
CHEMBL226636 Ki = 4.5 nM 8.35
CHEMBL390718 Ki = 8.3 nM 8.08
CHEMBL318235 Ki = 10.0 nM 8.00
CHEMBL226636 Ki = 23.0 nM 7.64
CHEMBL226636 Ki = 72.0 nM 7.14