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Assay Detail

CHEMBL822772

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Binding
Inhibition of alpha-1 adrenergic receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

From hit to lead. Analyzing structure-profile relationships.
Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Déprez B.
J Med Chem (2001) 44 : 3391 -3401
PubMed 11585444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.88 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114280 1 6.76
CHEMBL116463 1 6.38
CHEMBL113956 1 6.00
CHEMBL326263 1 5.96
CHEMBL114484 1 5.94
CHEMBL116735 1 5.93
CHEMBL114379 1 5.88
CHEMBL115444 1 5.87
CHEMBL325516 1 5.79
CHEMBL117537 1 5.66
CHEMBL115280 1 5.55
CHEMBL325750 1 5.37
CHEMBL420863 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114280 IC50 = 174.0 nM 6.76
CHEMBL116463 IC50 = 417.0 nM 6.38
CHEMBL113956 IC50 = 993.0 nM 6.00
CHEMBL326263 IC50 = 1100.0 nM 5.96
CHEMBL114484 IC50 = 1150.0 nM 5.94
CHEMBL116735 IC50 = 1170.0 nM 5.93
CHEMBL114379 IC50 = 1330.0 nM 5.88
CHEMBL115444 IC50 = 1340.0 nM 5.87
CHEMBL325516 IC50 = 1640.0 nM 5.79
CHEMBL117537 IC50 = 2190.0 nM 5.66
CHEMBL115280 IC50 = 2830.0 nM 5.55
CHEMBL325750 IC50 = 4250.0 nM 5.37
CHEMBL420863 IC50 = 4920.0 nM 5.31