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Assay Detail

CHEMBL1638262

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Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.
Sagratini G, Angeli P, Buccioni M, Gulini U, Marucci G, Melchiorre C, Poggesi E, Giardinà D.
Eur J Med Chem (2010) 45 : 5800 -5807
PubMed 20934789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 8.30 9.58
pKb 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630940 1 9.58
CHEMBL1630942 1 7.79
CHEMBL1630941 1 7.52
CHEMBL1630939 1 -
CHEMBL1630938 1 -
CHEMBL836 TAMSULOSIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630940 Kd = 0.263 nM 9.58
CHEMBL1630942 Kd = 16.22 nM 7.79
CHEMBL1630941 Kd = 30.2 nM 7.52
CHEMBL1630939 pKb = 9.66 -
CHEMBL1630938 pKb = 9.66 -
CHEMBL836 TAMSULOSIN pKb = 9.46 -