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Assay Detail

CHEMBL648056

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

Binding
In vitro alpha-2 adrenergic receptor binding affinity was determined on calf frontal cortex membrane preparation
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Frontal cortex
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.
Touzeau F, Arrault A, Guillaumet G, Scalbert E, Pfeiffer B, Rettori MC, Renard P, Mérour JY.
J Med Chem (2003) 46 : 1962 -1979
PubMed 12723959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.79 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13958 1 8.14
CHEMBL58187 1 7.98
CHEMBL62095 1 7.91
CHEMBL60031 1 7.58
CHEMBL13955 1 7.54
CHEMBL276035 1 7.52
CHEMBL14242 3 7.48
CHEMBL13810 1 7.28
CHEMBL13987 1 7.16
CHEMBL14028 1 7.13
CHEMBL267074 1 7.01
CHEMBL13940 1 6.88
CHEMBL13591 1 6.84
CHEMBL14110 1 6.84
CHEMBL13793 1 6.64
CHEMBL58186 1 6.58
CHEMBL274315 1 6.54
CHEMBL274784 1 6.47
CHEMBL60186 1 6.44
CHEMBL61689 1 6.40
CHEMBL13893 1 5.89
CHEMBL418716 1 5.67
CHEMBL14154 1 5.17
CHEMBL62107 1 5.12
CHEMBL13858 1 4.89
CHEMBL13938 1 -
CHEMBL13721 1 -
CHEMBL300388 1 -
CHEMBL13918 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13958 Ki = 7.3 nM 8.14
CHEMBL58187 Ki = 10.4 nM 7.98
CHEMBL62095 Ki = 12.4 nM 7.91
CHEMBL60031 Ki = 26.0 nM 7.58
CHEMBL13955 Ki = 28.6 nM 7.54
CHEMBL276035 Ki = 30.0 nM 7.52
CHEMBL14242 Ki = 32.9 nM 7.48
CHEMBL13810 Ki = 52.5 nM 7.28
CHEMBL14242 Ki = 68.2 nM 7.17
CHEMBL13987 Ki = 70.0 nM 7.16
CHEMBL14028 Ki = 74.0 nM 7.13
CHEMBL267074 Ki = 98.0 nM 7.01
CHEMBL14242 Ki = 104.0 nM 6.98
CHEMBL13940 Ki = 132.0 nM 6.88
CHEMBL14110 Ki = 145.0 nM 6.84
CHEMBL13591 Ki = 143.0 nM 6.84
CHEMBL13793 Ki = 230.0 nM 6.64
CHEMBL58186 Ki = 263.0 nM 6.58
CHEMBL274315 Ki = 287.0 nM 6.54
CHEMBL274784 Ki = 340.0 nM 6.47
CHEMBL60186 Ki = 360.0 nM 6.44
CHEMBL61689 Ki = 402.0 nM 6.40
CHEMBL13893 Ki = 1300.0 nM 5.89
CHEMBL418716 Ki = 2150.0 nM 5.67
CHEMBL14154 Ki = 6800.0 nM 5.17
CHEMBL62107 Ki = 7500.0 nM 5.12
CHEMBL13858 Ki = 13000.0 nM 4.89
CHEMBL13938 Ki > 1000.0 nM -
CHEMBL13721 Ki > 1000.0 nM -
CHEMBL300388 Ki > 1000.0 nM -
CHEMBL13918 Ki > 10000.0 nM -