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Assay Detail

CHEMBL646130

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

Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and adrenergic activities of ring-fluorinated epinephrines.
Adejare A, Gusovsky F, Padgett W, Creveling CR, Daly JW, Kirk KL.
J Med Chem (1988) 31 : 1972 -1977
PubMed 2845082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.53 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL679 EPINEPHRINE 4.0 1 6.40
CHEMBL42359 1 6.10
CHEMBL43711 1 5.48
CHEMBL287587 1 4.15
CHEMBL281232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL679 EPINEPHRINE EC50 = 400.0 nM 6.40
CHEMBL42359 EC50 = 800.0 nM 6.10
CHEMBL43711 EC50 = 3300.0 nM 5.48
CHEMBL287587 EC50 = 71000.0 nM 4.15
CHEMBL281232 EC50 = 125000.0 nM -