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Assay Detail

CHEMBL4826961

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

Binding
Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in post-mortem human brain frontal cortex membrane measured after 30 mins by liquid scintillation counting spectrometry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzofuranyl-2-imidazoles as imidazoline I<sub>2</sub> receptor ligands for Alzheimer's disease.
Rodriguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Pallàs M, Brocos-Mosquera I, Callado LF, Loza MI, Martínez AL, Brea J, Pérez B, Molins E, De Jonghe S, Daelemans D, Radan M, Djikic T, Nikolic K, Hernández-Hernández E, García-Fuster MJ, García-Sevilla JA, Escolano C.
Eur J Med Chem (2021) 222 : 113540 -113540
PubMed 34118720 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.52 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 8.35
CHEMBL4858960 1 4.92
CHEMBL404505 1 4.58
CHEMBL4857105 1 4.21
CHEMBL4861277 1 -
CHEMBL4866205 1 -
CHEMBL4861634 1 -
CHEMBL4857248 1 -
CHEMBL4856962 1 -
CHEMBL4859523 1 -
CHEMBL4855194 1 -
CHEMBL4864517 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Ki = 4.467 nM 8.35
CHEMBL4858960 Ki = 12022.64 nM 4.92
CHEMBL404505 Ki = 26302.68 nM 4.58
CHEMBL4857105 Ki = 61659.5 nM 4.21
CHEMBL4861277 Ki = 660693.45 nM -
CHEMBL4866205 Ki = 114815.36 nM -
CHEMBL4861634 Ki = 977237.22 nM -
CHEMBL4857248 Ki = 144543.98 nM -
CHEMBL4856962 Ki = 173780.08 nM -
CHEMBL4859523 Ki = 177827.94 nM -
CHEMBL4855194 Ki = 169824.37 nM -
CHEMBL4864517 Ki = 676082.98 nM -