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Assay Detail

CHEMBL643911

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

Binding
Displacement of [3H]rauwolscine from Alpha-2 adrenergic receptor of rat cortical membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.
Tagmatarchis N, Thermos K, Katerinopoulos HE.
J Med Chem (1998) 41 : 4165 -4170
PubMed 9767652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.05 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132304 1 9.30
CHEMBL134746 1 7.48
CHEMBL133432 1 7.17
CHEMBL134134 1 6.85
CHEMBL134903 1 6.81
CHEMBL132187 1 6.80
CHEMBL133431 1 6.71
CHEMBL336274 1 6.65
CHEMBL134273 1 6.60
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132304 IC50 = 0.5 nM 9.30
CHEMBL134746 IC50 = 33.0 nM 7.48
CHEMBL133432 IC50 = 67.5 nM 7.17
CHEMBL134134 IC50 = 142.0 nM 6.85
CHEMBL134903 IC50 = 154.0 nM 6.81
CHEMBL132187 IC50 = 160.0 nM 6.80
CHEMBL133431 IC50 = 197.0 nM 6.71
CHEMBL336274 IC50 = 226.0 nM 6.65
CHEMBL134273 IC50 = 251.0 nM 6.60
CHEMBL1437 NOREPINEPHRINE IC50 = 750.0 nM 6.12