Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL647723

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

Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
28
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Cid JM, De Lucas AI, Fernández J, Martínez S, Nieto C, Pastor J, Bakker MH, Biesmans I, Heylen LI, Megens AA.
Bioorg Med Chem Lett (2003) 13 : 2719 -2725
PubMed 12873501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.02 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419316 2 9.52
CHEMBL91157 2 9.52
CHEMBL90247 1 9.30
CHEMBL422597 1 9.10
CHEMBL93171 1 9.10
CHEMBL90943 1 9.05
CHEMBL92860 2 8.89
CHEMBL327875 1 8.85
CHEMBL268258 1 8.62
CHEMBL328114 2 8.59
CHEMBL94129 1 8.30
CHEMBL90997 1 8.23
CHEMBL93489 1 8.06
CHEMBL328735 1 7.92
CHEMBL328377 1 7.66
CHEMBL420830 1 7.64
CHEMBL90419 1 7.58
CHEMBL91824 1 7.47
CHEMBL93801 1 7.18
CHEMBL94435 1 7.01
CHEMBL90966 1 6.93
CHEMBL90843 1 6.73
CHEMBL92496 1 6.63
CHEMBL91297 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91157 Ki = 0.3 nM 9.52
CHEMBL419316 Ki = 0.3 nM 9.52
CHEMBL90247 Ki = 0.5 nM 9.30
CHEMBL422597 Ki = 0.8 nM 9.10
CHEMBL93171 Ki = 0.8 nM 9.10
CHEMBL90943 Ki = 0.9 nM 9.05
CHEMBL92860 Ki = 1.3 nM 8.89
CHEMBL327875 Ki = 1.4 nM 8.85
CHEMBL268258 Ki = 2.4 nM 8.62
CHEMBL328114 Ki = 2.6 nM 8.59
CHEMBL94129 Ki = 5.0 nM 8.30
CHEMBL90997 Ki = 5.9 nM 8.23
CHEMBL93489 Ki = 8.8 nM 8.06
CHEMBL328735 Ki = 12.0 nM 7.92
CHEMBL91157 Ki = 16.0 nM 7.80
CHEMBL328377 Ki = 22.0 nM 7.66
CHEMBL420830 Ki = 23.0 nM 7.64
CHEMBL328114 Ki = 25.0 nM 7.60
CHEMBL90419 Ki = 26.0 nM 7.58
CHEMBL419316 Ki = 30.0 nM 7.52
CHEMBL91824 Ki = 34.0 nM 7.47
CHEMBL93801 Ki = 66.0 nM 7.18
CHEMBL92860 Ki = 93.0 nM 7.03
CHEMBL94435 Ki = 98.0 nM 7.01
CHEMBL90966 Ki = 117.0 nM 6.93
CHEMBL90843 Ki = 186.0 nM 6.73
CHEMBL92496 Ki = 234.0 nM 6.63
CHEMBL91297 Ki = 234.0 nM 6.63