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Assay Detail

CHEMBL822168

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

Binding
Binding of [3H]clonidine to alpha-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 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
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 21 7.21 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40986 1 7.89
CHEMBL679 EPINEPHRINE 4.0 2 7.89
CHEMBL42359 1 7.85
CHEMBL40317 1 7.70
CHEMBL1437 NOREPINEPHRINE 4.0 3 7.70
CHEMBL281232 1 7.55
CHEMBL41818 1 7.40
CHEMBL42280 L-ADRENALINE 1 7.35
CHEMBL295651 1 7.28
CHEMBL59 DOPAMINE 4.0 1 7.24
CHEMBL43711 1 7.22
CHEMBL42370 1 7.17
CHEMBL42216 1 7.11
CHEMBL40268 1 6.92
CHEMBL40796 1 6.50
CHEMBL40593 1 6.44
CHEMBL295072 1 6.26
CHEMBL287587 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL679 EPINEPHRINE Ki = 13.0 nM 7.89
CHEMBL40986 Ki = 13.0 nM 7.89
CHEMBL42359 Ki = 14.0 nM 7.85
CHEMBL679 EPINEPHRINE Ki = 15.0 nM 7.82
CHEMBL1437 NOREPINEPHRINE Ki = 20.0 nM 7.70
CHEMBL40317 Ki = 20.0 nM 7.70
CHEMBL281232 Ki = 28.0 nM 7.55
CHEMBL1437 NOREPINEPHRINE Ki = 30.0 nM 7.52
CHEMBL41818 Ki = 40.0 nM 7.40
CHEMBL42280 L-ADRENALINE Ki = 45.0 nM 7.35
CHEMBL295651 Ki = 53.0 nM 7.28
CHEMBL59 DOPAMINE Ki = 58.0 nM 7.24
CHEMBL43711 Ki = 60.0 nM 7.22
CHEMBL42370 Ki = 67.0 nM 7.17
CHEMBL42216 Ki = 78.0 nM 7.11
CHEMBL40268 Ki = 120.0 nM 6.92
CHEMBL40796 Ki = 320.0 nM 6.50
CHEMBL1437 NOREPINEPHRINE Ki = 340.0 nM 6.47
CHEMBL40593 Ki = 360.0 nM 6.44
CHEMBL295072 Ki = 550.0 nM 6.26
CHEMBL287587 Ki = 600.0 nM 6.22