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Assay Detail

CHEMBL891161

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

Functional
Antagonist activity against adrenergic Alpha-1B receptor in rat spleen assessed as inhibition of phenylephrine-induced response
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Spleen
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1B adrenergic receptor (CHEMBL315)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Sagratini G, Angeli P, Buccioni M, Gulini U, Marucci G, Melchiorre C, Leonardi A, Poggesi E, Giardinà D.
Bioorg Med Chem (2007) 15 : 2334 -2345
PubMed 17276073 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pKb 8 - -
Kd 1 8.65 8.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242507 1 8.65
CHEMBL423294 CYCLAZOSIN 1 -
CHEMBL242934 1 -
CHEMBL242725 1 -
CHEMBL389978 1 -
CHEMBL242724 1 -
CHEMBL242723 1 -
CHEMBL242508 1 -
CHEMBL388884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242507 Kd = 2.239 nM 8.65
CHEMBL423294 CYCLAZOSIN pKb = 8.86 -
CHEMBL242934 pKb = 8.83 -
CHEMBL242725 pKb = 8.64 -
CHEMBL389978 pKb = 8.05 -
CHEMBL242724 pKb = 8.78 -
CHEMBL242723 pKb = 8.13 -
CHEMBL242508 pKb = 8.5 -
CHEMBL388884 pKb = 8.5 -