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Assay Detail

CHEMBL973553

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

Binding
Displacement of [3H]RX821002 from Adrenergic alpha2 receptor in Sprague-Dawley rat whole brain membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.
Gentili F, Cardinaletti C, Vesprini C, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Mattioli L, Perfumi M, Hudson A, Pigini M.
J Med Chem (2008) 51 : 5130 -5134
PubMed 18661965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.82 6.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL498476 1 6.53
CHEMBL506016 1 6.53
CHEMBL497458 1 6.42
CHEMBL450405 1 6.25
CHEMBL508960 1 6.09
CHEMBL498261 1 6.03
CHEMBL525531 1 5.95
CHEMBL14210 PHENYZOLINE 1 5.70
CHEMBL506350 1 5.53
CHEMBL448918 1 5.45
CHEMBL501690 1 5.15
CHEMBL452401 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL498476 Ki = 292.7 nM 6.53
CHEMBL506016 Ki = 295.4 nM 6.53
CHEMBL497458 Ki = 381.0 nM 6.42
CHEMBL450405 Ki = 557.7 nM 6.25
CHEMBL508960 Ki = 819.9 nM 6.09
CHEMBL498261 Ki = 925.9 nM 6.03
CHEMBL525531 Ki = 1117.9 nM 5.95
CHEMBL14210 PHENYZOLINE Ki = 1985.0 nM 5.70
CHEMBL506350 Ki = 2962.0 nM 5.53
CHEMBL448918 Ki = 3540.0 nM 5.45
CHEMBL501690 Ki = 7132.0 nM 5.15
CHEMBL452401 Ki = 64773.0 nM 4.19