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Assay Detail

CHEMBL841870

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

Binding
Displacement of [3H]idazoxan from imidazoline receptor I-2 binding sites in rabbit kidney membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Kidney
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Monoamine oxidase (CHEMBL2095205)
Type PROTEIN FAMILY
Organism Homo sapiens

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 6.15 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14640 1 9.05
CHEMBL13881 PHENAMAZOLINE 2.0 1 7.48
CHEMBL337945 1 6.74
CHEMBL13925 1 6.70
CHEMBL131775 1 6.57
CHEMBL13789 1 6.52
CHEMBL337862 1 6.09
CHEMBL128168 BIPHENYLINE 1 5.79
CHEMBL273485 1 5.57
CHEMBL396013 1 5.14
CHEMBL131222 1 5.12
CHEMBL130884 1 4.90
CHEMBL242265 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14640 Ki = 0.8913 nM 9.05
CHEMBL13881 PHENAMAZOLINE Ki = 33.11 nM 7.48
CHEMBL337945 Ki = 181.97 nM 6.74
CHEMBL13925 Ki = 199.53 nM 6.70
CHEMBL131775 Ki = 269.15 nM 6.57
CHEMBL13789 Ki = 302.0 nM 6.52
CHEMBL337862 Ki = 812.83 nM 6.09
CHEMBL128168 BIPHENYLINE Ki = 1621.81 nM 5.79
CHEMBL273485 Ki = 2691.53 nM 5.57
CHEMBL396013 Ki = 7244.36 nM 5.14
CHEMBL131222 Ki = 7585.78 nM 5.12
CHEMBL130884 Ki = 12589.25 nM 4.90
CHEMBL242265 Ki = 48977.88 nM 4.31