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Assay Detail

CHEMBL645211

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

Binding
Displacement of [3H]clonidine from rat cortex membrane Alpha-2 adrenergic receptors
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.
Gentili F, Bousquet P, Brasili L, Dontenwill M, Feldman J, Ghelfi F, Giannella M, Piergentili A, Quaglia W, Pigini M.
J Med Chem (2003) 46 : 2169 -2176
PubMed 12747788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.04 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14640 1 7.28
CHEMBL273485 1 7.01
CHEMBL93845 1 6.92
CHEMBL94022 1 6.62
CHEMBL67706 1 6.40
CHEMBL68608 1 5.93
CHEMBL1907831 1 5.90
CHEMBL2092860 1 5.80
CHEMBL14210 PHENYZOLINE 1 5.70
CHEMBL71429 1 5.45
CHEMBL1907832 1 5.40
CHEMBL2092861 1 5.30
CHEMBL275970 TRACIZOLINE 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14640 Ki = 52.48 nM 7.28
CHEMBL273485 Ki = 97.72 nM 7.01
CHEMBL93845 Ki = 120.23 nM 6.92
CHEMBL94022 Ki = 239.88 nM 6.62
CHEMBL67706 Ki = 398.11 nM 6.40
CHEMBL68608 Ki = 1174.9 nM 5.93
CHEMBL1907831 Ki = 1258.93 nM 5.90
CHEMBL2092860 Ki = 1584.89 nM 5.80
CHEMBL14210 PHENYZOLINE Ki = 1995.26 nM 5.70
CHEMBL71429 Ki = 3548.13 nM 5.45
CHEMBL1907832 Ki = 3981.07 nM 5.40
CHEMBL2092861 Ki = 5011.87 nM 5.30
CHEMBL275970 TRACIZOLINE Ki = 14125.38 nM 4.85