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Assay Detail

CHEMBL649240

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

Binding
Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-2C adrenergic receptor (CHEMBL1916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.
Kennis LE, Bischoff FP, Mertens CJ, Love CJ, Van den Keybus FA, Pieters S, Braeken M, Megens AA, Leysen JE.
Bioorg Med Chem Lett (2000) 10 : 71 -74
PubMed 10636247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.49 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162682 1 9.21
CHEMBL165350 1 9.16
CHEMBL162490 1 9.15
CHEMBL351483 1 9.14
CHEMBL162232 1 9.07
CHEMBL163190 1 8.97
CHEMBL165796 1 8.92
CHEMBL162370 1 8.89
CHEMBL351200 1 8.88
CHEMBL163247 1 8.87
CHEMBL162826 1 8.79
CHEMBL162501 LUSAPERIDONE 2.0 1 8.77
CHEMBL164612 1 8.65
CHEMBL162436 1 8.57
CHEMBL162147 1 8.44
CHEMBL165776 1 8.18
CHEMBL165181 1 7.85
CHEMBL165677 1 7.56
CHEMBL10316 IDAZOXAN 3.0 1 7.27
CHEMBL162058 1 7.24
CHEMBL654 MIRTAZAPINE 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162682 IC50 = 0.6166 nM 9.21
CHEMBL165350 IC50 = 0.6918 nM 9.16
CHEMBL162490 IC50 = 0.7079 nM 9.15
CHEMBL351483 IC50 = 0.7244 nM 9.14
CHEMBL162232 IC50 = 0.8511 nM 9.07
CHEMBL163190 IC50 = 1.072 nM 8.97
CHEMBL165796 IC50 = 1.202 nM 8.92
CHEMBL162370 IC50 = 1.288 nM 8.89
CHEMBL351200 IC50 = 1.318 nM 8.88
CHEMBL163247 IC50 = 1.349 nM 8.87
CHEMBL162826 IC50 = 1.622 nM 8.79
CHEMBL162501 LUSAPERIDONE IC50 = 1.698 nM 8.77
CHEMBL164612 IC50 = 2.239 nM 8.65
CHEMBL162436 IC50 = 2.692 nM 8.57
CHEMBL162147 IC50 = 3.631 nM 8.44
CHEMBL165776 IC50 = 6.607 nM 8.18
CHEMBL165181 IC50 = 14.13 nM 7.85
CHEMBL165677 IC50 = 27.54 nM 7.56
CHEMBL10316 IDAZOXAN IC50 = 53.7 nM 7.27
CHEMBL162058 IC50 = 57.54 nM 7.24
CHEMBL654 MIRTAZAPINE IC50 = 199.53 nM 6.70