Assay Detail

CHEMBL644676

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Functional

In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens

ChEMBL ↗

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Target

Alpha-1A adrenergic receptor (CHEMBL319) ↗

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Alpha-1A adrenergic receptor (CHEMBL319) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Alpha-1A adrenergic receptor

CHEMBL319

Anchored from Assay target.

Protein identity Alpha-1A adrenergic receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Tissue	Vas deferens
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prostatic hyperplasia.

Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Drizin I, Elmore SW, Ehrlich PP, Lebold SA, Tietje K, Sippy KB, Wendt MD, Plata DJ, Plagge F, Buckner SA, Brune ME, Hancock AA, Kerwin JF.
J Med Chem (1997) 40 : 3141 -3143
PubMed 9379432 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	3	8.81	9.47

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL836	TAMSULOSIN	4.0	1	9.47
CHEMBL40650	—	—	1	8.93
CHEMBL611	TERAZOSIN	4.0	1	8.04

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL836	TAMSULOSIN	Kd	=	0.3388	nM	9.47
CHEMBL40650	—	Kd	=	1.175	nM	8.93
CHEMBL611	TERAZOSIN	Kd	=	9.12	nM	8.04