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Assay Detail

CHEMBL3106122

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

Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
Rajagopalan R, Bandyopadhyaya A, Rajagopalan DR, Rajagopalan P.
Bioorg Med Chem Lett (2014) 24 : 576 -579
PubMed 24365159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.97 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL762 OXYMETAZOLINE 4.0 2 9.54
CHEMBL3104091 2 6.64
CHEMBL3104093 2 6.39
CHEMBL3104092 2 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL762 OXYMETAZOLINE Ki = 0.29 nM 9.54
CHEMBL762 OXYMETAZOLINE Ki = 2.291 nM 8.64
CHEMBL3104091 Ki = 228.0 nM 6.64
CHEMBL3104091 Ki = 229.09 nM 6.64
CHEMBL3104093 Ki = 407.0 nM 6.39
CHEMBL3104093 Ki = 407.38 nM 6.39
CHEMBL3104092 Ki = 1800.0 nM 5.75
CHEMBL3104092 Ki = 1819.7 nM 5.74