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Assay Detail

CHEMBL640225

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

Binding
Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat cortex membrane
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

Alpha2-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole.
Gentili F, Bousquet P, Brasili L, Caretto M, Carrieri A, Dontenwill M, Giannella M, Marucci G, Perfumi M, Piergentili A, Quaglia W, Rascente C, Pigini M.
J Med Chem (2002) 45 : 32 -40
PubMed 11754577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.09 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128168 BIPHENYLINE 1 7.91
CHEMBL396013 1 7.50
CHEMBL337945 1 7.50
CHEMBL14640 1 7.28
CHEMBL13881 PHENAMAZOLINE 2.0 1 7.14
CHEMBL13789 1 7.10
CHEMBL273485 1 7.01
CHEMBL242265 1 7.00
CHEMBL130884 1 7.00
CHEMBL131775 1 6.92
CHEMBL131222 1 6.80
CHEMBL13925 1 6.52
CHEMBL337862 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128168 BIPHENYLINE Ki = 12.3 nM 7.91
CHEMBL396013 Ki = 31.62 nM 7.50
CHEMBL337945 Ki = 31.62 nM 7.50
CHEMBL14640 Ki = 52.48 nM 7.28
CHEMBL13881 PHENAMAZOLINE Ki = 72.44 nM 7.14
CHEMBL13789 Ki = 79.43 nM 7.10
CHEMBL273485 Ki = 97.72 nM 7.01
CHEMBL242265 Ki = 100.0 nM 7.00
CHEMBL130884 Ki = 100.0 nM 7.00
CHEMBL131775 Ki = 120.23 nM 6.92
CHEMBL131222 Ki = 158.49 nM 6.80
CHEMBL13925 Ki = 302.0 nM 6.52
CHEMBL337862 Ki = 354.81 nM 6.45