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Assay Detail

CHEMBL3421397

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

Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
Huang J, He F, Huang M, Liu X, Xiong Y, Huang Y, Zhu L, Yang Y, Xu X, Yuan M.
Eur J Med Chem (2015) 96 : 83 -91
PubMed 25874333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 7.47 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415020 1 8.13
CHEMBL3415012 1 8.10
CHEMBL3415014 1 7.90
CHEMBL611 TERAZOSIN 4.0 1 7.90
CHEMBL3415011 1 7.58
CHEMBL142635 NAFTOPIDIL 4.0 1 7.48
CHEMBL3415018 1 7.32
CHEMBL3415019 1 7.28
CHEMBL3415015 1 7.26
CHEMBL3415016 1 7.23
CHEMBL3415017 1 7.16
CHEMBL3414578 1 7.11
CHEMBL3415013 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415020 Kd = 7.413 nM 8.13
CHEMBL3415012 Kd = 7.943 nM 8.10
CHEMBL3415014 Kd = 12.59 nM 7.90
CHEMBL611 TERAZOSIN Kd = 12.59 nM 7.90
CHEMBL3415011 Kd = 26.3 nM 7.58
CHEMBL142635 NAFTOPIDIL Kd = 33.11 nM 7.48
CHEMBL3415018 Kd = 47.86 nM 7.32
CHEMBL3415019 Kd = 52.48 nM 7.28
CHEMBL3415015 Kd = 54.95 nM 7.26
CHEMBL3415016 Kd = 58.88 nM 7.23
CHEMBL3415017 Kd = 69.18 nM 7.16
CHEMBL3414578 Kd = 77.62 nM 7.11
CHEMBL3415013 Kd = 194.98 nM 6.71