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Assay Detail

CHEMBL643739

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

Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
20
Total Activities
20
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-1A adrenergic receptor (CHEMBL229)
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 20 6.22 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL165796 1 6.95
CHEMBL162490 1 6.94
CHEMBL162436 1 6.69
CHEMBL165181 1 6.67
CHEMBL162232 1 6.62
CHEMBL162826 1 6.61
CHEMBL164612 1 6.55
CHEMBL162370 1 6.54
CHEMBL162501 LUSAPERIDONE 2.0 1 6.46
CHEMBL163190 1 6.40
CHEMBL162682 1 6.32
CHEMBL351200 1 6.16
CHEMBL351483 1 6.14
CHEMBL165776 1 6.09
CHEMBL165350 1 6.05
CHEMBL163247 1 5.59
CHEMBL10316 IDAZOXAN 3.0 1 5.54
CHEMBL654 MIRTAZAPINE 4.0 1 5.50
CHEMBL162058 1 5.28
CHEMBL162147 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL165796 IC50 = 112.2 nM 6.95
CHEMBL162490 IC50 = 114.82 nM 6.94
CHEMBL162436 IC50 = 204.17 nM 6.69
CHEMBL165181 IC50 = 213.8 nM 6.67
CHEMBL162232 IC50 = 239.88 nM 6.62
CHEMBL162826 IC50 = 245.47 nM 6.61
CHEMBL164612 IC50 = 281.84 nM 6.55
CHEMBL162370 IC50 = 288.4 nM 6.54
CHEMBL162501 LUSAPERIDONE IC50 = 346.74 nM 6.46
CHEMBL163190 IC50 = 398.11 nM 6.40
CHEMBL162682 IC50 = 478.63 nM 6.32
CHEMBL351200 IC50 = 691.83 nM 6.16
CHEMBL351483 IC50 = 724.44 nM 6.14
CHEMBL165776 IC50 = 812.83 nM 6.09
CHEMBL165350 IC50 = 891.25 nM 6.05
CHEMBL163247 IC50 = 2570.4 nM 5.59
CHEMBL10316 IDAZOXAN IC50 = 2884.03 nM 5.54
CHEMBL654 MIRTAZAPINE IC50 = 3162.28 nM 5.50
CHEMBL162058 IC50 = 5248.07 nM 5.28
CHEMBL162147 IC50 = 5888.44 nM 5.23