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Assay Detail

CHEMBL653363

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

Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-1 adrenergic receptor (CHEMBL5471)
Type SINGLE PROTEIN
Organism Cavia porcellus

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
Ki 6 5.67 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287587 1 6.46
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.40
CHEMBL43711 1 5.75
CHEMBL679 EPINEPHRINE 4.0 1 5.52
CHEMBL42359 1 4.20
CHEMBL281232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287587 Ki = 350.0 nM 6.46
CHEMBL1437 NOREPINEPHRINE Ki = 400.0 nM 6.40
CHEMBL43711 Ki = 1800.0 nM 5.75
CHEMBL679 EPINEPHRINE Ki = 3000.0 nM 5.52
CHEMBL42359 Ki = 63000.0 nM 4.20
CHEMBL281232 Ki > 3000.0 nM -