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Assay Detail

CHEMBL1052925

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

Binding
Displacement of [3H]Clonidine from alpha2 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
Groszek G, Nowak-Król A, Wdowik T, Swierczyński D, Bednarski M, Otto M, Walczak M, Filipek B.
Eur J Med Chem (2009) 44 : 5103 -5111
PubMed 19647907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.43 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477465 1 8.85
CHEMBL723 CARVEDILOL 4.0 1 8.47
CHEMBL572571 1 7.37
CHEMBL573946 1 7.25
CHEMBL573951 1 7.21
CHEMBL582863 1 6.96
CHEMBL574593 1 6.74
CHEMBL573945 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477465 Ki = 1.4 nM 8.85
CHEMBL723 CARVEDILOL Ki = 3.4 nM 8.47
CHEMBL572571 Ki = 43.0 nM 7.37
CHEMBL573946 Ki = 56.9 nM 7.25
CHEMBL573951 Ki = 60.9 nM 7.21
CHEMBL582863 Ki = 108.8 nM 6.96
CHEMBL574593 Ki = 180.8 nM 6.74
CHEMBL573945 Ki = 277.2 nM 6.56