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Assay Detail

CHEMBL648169

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

Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].
Cordi AA, Lacoste JM, Descombes JJ, Courchay C, Vanhoutte PM, Laubie M, Verbeuren TJ.
J Med Chem (1995) 38 : 4056 -4069
PubMed 7562941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.62 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133231 1 8.80
CHEMBL338683 1 8.52
CHEMBL98471 1 8.15
CHEMBL336332 1 7.92
CHEMBL131220 1 7.92
CHEMBL130853 1 7.47
CHEMBL133579 1 7.29
CHEMBL131417 1 7.29
CHEMBL336970 1 7.06
CHEMBL101340 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133231 Ki = 1.6 nM 8.80
CHEMBL338683 Ki = 3.0 nM 8.52
CHEMBL98471 Ki = 7.0 nM 8.15
CHEMBL336332 Ki = 12.0 nM 7.92
CHEMBL131220 Ki = 12.0 nM 7.92
CHEMBL130853 Ki = 34.0 nM 7.47
CHEMBL133579 Ki = 51.0 nM 7.29
CHEMBL131417 Ki = 51.0 nM 7.29
CHEMBL336970 Ki = 87.0 nM 7.06
CHEMBL101340 Ki = 1560.0 nM 5.81