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Assay Detail

CHEMBL857029

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

Functional
The compound was evaluated for the alpha-1 adrenergic receptor antagonistic activity in rat vas deferens vs methoxamine alpha-1 adrenoceptor antagonism
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
Hlasta DJ, Luttinger D, Perrone MH, Silbernagel MJ, Ward SJ, Haubrich DR.
J Med Chem (1987) 30 : 1555 -1562
PubMed 2887657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.56 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41720 1 8.03
CHEMBL416072 1 8.02
CHEMBL38829 1 7.75
CHEMBL10316 IDAZOXAN 3.0 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41720 Kd = 9.333 nM 8.03
CHEMBL416072 Kd = 9.55 nM 8.02
CHEMBL38829 Kd = 17.78 nM 7.75
CHEMBL10316 IDAZOXAN Kd = 380.19 nM 6.42