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Assay Detail

CHEMBL644563

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

Functional
Antagonist potency towards alpha-1 adrenergic receptor in the rat electrically stimulated vas deferens with reference to phenylephrine
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

Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
Stillings MR, England CD, Welbourn AP, Smith CF.
J Med Chem (1986) 29 : 1780 -1783
PubMed 2875186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.96 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10332 1 7.43
CHEMBL31836 PIPEROXAN 2.0 1 7.16
CHEMBL10316 IDAZOXAN 3.0 1 6.30
CHEMBL52429 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10332 Kd = 37.15 nM 7.43
CHEMBL31836 PIPEROXAN Kd = 69.18 nM 7.16
CHEMBL10316 IDAZOXAN Kd = 501.19 nM 6.30
CHEMBL52429 Kd > 33113.11 nM -