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Assay Detail

CHEMBL649436

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

Binding
Binding affinity for alpha-1 adrenergic receptor in rat liver using [3H]prazosin.
5
Total Activities
5
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 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.
DeBernardis JF, Kerkman DJ, Arendsen DL, Buckner SA, Kyncl JJ, Hancock AA.
J Med Chem (1987) 30 : 1011 -1017
PubMed 2884313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.29 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.41
CHEMBL7186 1 6.40
CHEMBL7707 1 6.28
CHEMBL134 CLONIDINE 4.0 1 6.28
CHEMBL7169 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1437 NOREPINEPHRINE Ki = 390.0 nM 6.41
CHEMBL7186 Ki = 400.0 nM 6.40
CHEMBL7707 Ki = 523.0 nM 6.28
CHEMBL134 CLONIDINE Ki = 520.0 nM 6.28
CHEMBL7169 Ki = 817.0 nM 6.09