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Assay Detail

CHEMBL842748

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

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

Assay Information

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

Target

Monoamine oxidase (CHEMBL2095205)
Type PROTEIN FAMILY
Organism Homo sapiens

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 7.08 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14640 1 9.05
CHEMBL275970 TRACIZOLINE 1 8.72
CHEMBL14210 PHENYZOLINE 1 8.60
CHEMBL93845 1 8.22
CHEMBL67706 1 7.64
CHEMBL2092860 1 7.00
CHEMBL94022 1 6.91
CHEMBL68608 1 6.91
CHEMBL2092861 1 6.84
CHEMBL71429 1 6.03
CHEMBL1907831 1 5.60
CHEMBL273485 1 5.57
CHEMBL1907832 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14640 Ki = 0.8913 nM 9.05
CHEMBL275970 TRACIZOLINE Ki = 1.905 nM 8.72
CHEMBL14210 PHENYZOLINE Ki = 2.512 nM 8.60
CHEMBL93845 Ki = 6.026 nM 8.22
CHEMBL67706 Ki = 22.91 nM 7.64
CHEMBL2092860 Ki = 100.0 nM 7.00
CHEMBL94022 Ki = 123.03 nM 6.91
CHEMBL68608 Ki = 123.03 nM 6.91
CHEMBL2092861 Ki = 144.54 nM 6.84
CHEMBL71429 Ki = 933.25 nM 6.03
CHEMBL1907831 Ki = 2511.89 nM 5.60
CHEMBL273485 Ki = 2691.53 nM 5.57
CHEMBL1907832 Ki = 12589.25 nM 4.90