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Assay Detail

CHEMBL647965

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

Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Munk SA, Harcourt DA, Arasasingham PN, Burke JA, Kharlamb AB, Manlapaz CA, Padillo EU, Roberts D, Runde E, Williams L, Wheeler LA, Garst ME.
J Med Chem (1997) 40 : 18 -23
PubMed 9016324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.50 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308570 1 8.77
CHEMBL49137 1 8.70
CHEMBL844 BRIMONIDINE 4.0 1 8.57
CHEMBL75257 1 8.31
CHEMBL432155 1 8.22
CHEMBL77913 1 8.00
CHEMBL75491 1 7.51
CHEMBL78190 1 7.41
CHEMBL74544 1 7.12
CHEMBL1022 1 7.02
CHEMBL308863 1 6.89
CHEMBL76457 1 6.68
CHEMBL1019 1 6.29
CHEMBL74449 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308570 Ki = 1.7 nM 8.77
CHEMBL49137 Ki = 2.0 nM 8.70
CHEMBL844 BRIMONIDINE Ki = 2.7 nM 8.57
CHEMBL75257 Ki = 4.9 nM 8.31
CHEMBL432155 Ki = 6.0 nM 8.22
CHEMBL77913 Ki = 10.0 nM 8.00
CHEMBL75491 Ki = 31.0 nM 7.51
CHEMBL78190 Ki = 39.0 nM 7.41
CHEMBL74544 Ki = 76.0 nM 7.12
CHEMBL1022 Ki = 95.0 nM 7.02
CHEMBL308863 Ki = 130.0 nM 6.89
CHEMBL76457 Ki = 210.0 nM 6.68
CHEMBL1019 Ki = 510.0 nM 6.29
CHEMBL74449 Ki = 3100.0 nM 5.51