Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL645548

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

Binding
Binding of [3H]prazosin to alpha-1 adrenergic receptor of rat cerebral cortical membranes
18
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 18 5.33 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL679 EPINEPHRINE 4.0 2 5.80
CHEMBL40986 1 5.60
CHEMBL1437 NOREPINEPHRINE 4.0 2 5.52
CHEMBL40317 1 5.43
CHEMBL42359 1 5.30
CHEMBL41818 1 5.22
CHEMBL59 DOPAMINE 4.0 1 4.85
CHEMBL40268 1 4.80
CHEMBL295651 1 -
CHEMBL287587 1 -
CHEMBL42280 L-ADRENALINE 1 -
CHEMBL42216 1 -
CHEMBL42370 1 -
CHEMBL295072 1 -
CHEMBL43711 1 -
CHEMBL40593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL679 EPINEPHRINE Ki = 1600.0 nM 5.80
CHEMBL40986 Ki = 2500.0 nM 5.60
CHEMBL679 EPINEPHRINE Ki = 2800.0 nM 5.55
CHEMBL1437 NOREPINEPHRINE Ki = 3000.0 nM 5.52
CHEMBL40317 Ki = 3700.0 nM 5.43
CHEMBL42359 Ki = 5000.0 nM 5.30
CHEMBL41818 Ki = 6000.0 nM 5.22
CHEMBL1437 NOREPINEPHRINE Ki = 6500.0 nM 5.19
CHEMBL59 DOPAMINE Ki = 14000.0 nM 4.85
CHEMBL40268 Ki = 16000.0 nM 4.80
CHEMBL295072 Ki ~ 25000.0 nM -
CHEMBL40593 Ki ~ 12000.0 nM -
CHEMBL43711 Ki ~ 25000.0 nM -
CHEMBL295651 Ki ~ 40000.0 nM -
CHEMBL42370 Ki ~ 25000.0 nM -
CHEMBL42216 Ki ~ 70000.0 nM -
CHEMBL42280 L-ADRENALINE Ki ~ 20000.0 nM -
CHEMBL287587 Ki ~ 50000.0 nM -