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Assay Detail

CHEMBL652293

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

Binding
Binding of [3H]dihydroalprenolol to beta-2 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-2 adrenergic receptor (CHEMBL2289)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

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 5.35 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL295072 1 7.17
CHEMBL42370 1 6.96
CHEMBL287587 1 6.85
CHEMBL43711 1 6.58
CHEMBL679 EPINEPHRINE 4.0 2 6.18
CHEMBL42280 L-ADRENALINE 1 5.43
CHEMBL1437 NOREPINEPHRINE 4.0 3 5.30
CHEMBL295651 1 4.62
CHEMBL40796 1 4.57
CHEMBL40317 1 4.55
CHEMBL40986 1 4.42
CHEMBL59 DOPAMINE 4.0 1 4.30
CHEMBL42359 1 4.30
CHEMBL281232 1 4.24
CHEMBL40268 1 -
CHEMBL40593 1 -
CHEMBL42216 1 -
CHEMBL41818 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL295072 Ki = 67.0 nM 7.17
CHEMBL42370 Ki = 110.0 nM 6.96
CHEMBL287587 Ki = 140.0 nM 6.85
CHEMBL43711 Ki = 260.0 nM 6.58
CHEMBL679 EPINEPHRINE Ki = 660.0 nM 6.18
CHEMBL679 EPINEPHRINE Ki = 1100.0 nM 5.96
CHEMBL42280 L-ADRENALINE Ki = 3700.0 nM 5.43
CHEMBL1437 NOREPINEPHRINE Ki = 5000.0 nM 5.30
CHEMBL1437 NOREPINEPHRINE Ki = 11000.0 nM 4.96
CHEMBL295651 Ki = 24000.0 nM 4.62
CHEMBL1437 NOREPINEPHRINE Ki = 27000.0 nM 4.57
CHEMBL40796 Ki = 27000.0 nM 4.57
CHEMBL40317 Ki = 28000.0 nM 4.55
CHEMBL40986 Ki = 38000.0 nM 4.42
CHEMBL59 DOPAMINE Ki = 50000.0 nM 4.30
CHEMBL42359 Ki = 50000.0 nM 4.30
CHEMBL281232 Ki = 58000.0 nM 4.24
CHEMBL40268 Ki ~ 70000.0 nM -
CHEMBL40593 Ki ~ 270000.0 nM -
CHEMBL42216 Ki ~ 90000.0 nM -
CHEMBL41818 Ki ~ 130000.0 nM -