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Assay Detail

CHEMBL647622

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

Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
21
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-1 adrenergic receptor (CHEMBL3252)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.
Lu SF, Herbert B, Haufe G, Laue KW, Padgett WL, Oshunleti O, Daly JW, Kirk KL.
J Med Chem (2000) 43 : 1611 -1619
PubMed 10780918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.33 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL295072 1 6.89
CHEMBL287587 1 6.68
CHEMBL42370 1 6.25
CHEMBL679 EPINEPHRINE 4.0 2 5.96
CHEMBL1437 NOREPINEPHRINE 4.0 3 5.89
CHEMBL43711 1 5.75
CHEMBL59 DOPAMINE 4.0 1 5.00
CHEMBL42280 L-ADRENALINE 1 4.89
CHEMBL40268 1 4.72
CHEMBL40317 1 4.62
CHEMBL41818 1 4.39
CHEMBL40796 1 4.28
CHEMBL281232 1 4.20
CHEMBL42216 1 -
CHEMBL42359 1 -
CHEMBL40986 1 -
CHEMBL295651 1 -
CHEMBL40593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL295072 Ki = 130.0 nM 6.89
CHEMBL287587 Ki = 210.0 nM 6.68
CHEMBL42370 Ki = 560.0 nM 6.25
CHEMBL679 EPINEPHRINE Ki = 1100.0 nM 5.96
CHEMBL1437 NOREPINEPHRINE Ki = 1300.0 nM 5.89
CHEMBL43711 Ki = 1800.0 nM 5.75
CHEMBL679 EPINEPHRINE Ki = 2100.0 nM 5.68
CHEMBL1437 NOREPINEPHRINE Ki = 2700.0 nM 5.57
CHEMBL59 DOPAMINE Ki = 10000.0 nM 5.00
CHEMBL42280 L-ADRENALINE Ki = 13000.0 nM 4.89
CHEMBL40268 Ki = 19000.0 nM 4.72
CHEMBL40317 Ki = 24000.0 nM 4.62
CHEMBL1437 NOREPINEPHRINE Ki = 26000.0 nM 4.58
CHEMBL41818 Ki = 41000.0 nM 4.39
CHEMBL40796 Ki = 52000.0 nM 4.28
CHEMBL281232 Ki = 63000.0 nM 4.20
CHEMBL42359 Ki ~ 140000.0 nM -
CHEMBL42216 Ki ~ 400000.0 nM -
CHEMBL40986 Ki ~ 100000.0 nM -
CHEMBL295651 Ki ~ 150000.0 nM -
CHEMBL40593 Ki ~ 120000.0 nM -