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Assay Detail

CHEMBL984238

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

Binding
Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane after 30 mins by liquid scintillation spectrometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Prefrontal cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor ligands: searching for structure-activity relationships.
Rodriguez F, Rozas I, Ortega JE, Erdozain AM, Meana JJ, Callado LF, Callado LF.
J Med Chem (2009) 52 : 601 -609
PubMed 19133776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.34 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10332 1 9.04
CHEMBL134 CLONIDINE 4.0 1 7.68
CHEMBL473567 1 7.38
CHEMBL10316 IDAZOXAN 3.0 1 7.29
CHEMBL467525 1 7.27
CHEMBL482359 1 7.12
CHEMBL509581 1 6.95
CHEMBL506313 1 6.75
CHEMBL498849 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10332 Ki = 0.912 nM 9.04
CHEMBL134 CLONIDINE Ki = 20.89 nM 7.68
CHEMBL473567 Ki = 41.69 nM 7.38
CHEMBL10316 IDAZOXAN Ki = 51.29 nM 7.29
CHEMBL467525 Ki = 53.7 nM 7.27
CHEMBL482359 Ki = 75.86 nM 7.12
CHEMBL509581 Ki = 112.2 nM 6.95
CHEMBL506313 Ki = 177.83 nM 6.75
CHEMBL498849 Ki = 263.03 nM 6.58