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Assay Detail

CHEMBL645607

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

Binding
Binding affinity for Alpha-2 adrenergic receptor of CHO-C10 membrane preparation
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Analogs of UK 14,304: Structural features responsible for 2 adrenoceptor activity
Munk S, Harcourt D, Arasasingham P, Gluchowski C, Wong H, Burke J, Kharlamb A, Manlapaz C, Padillo E, Williams L, Wheeler L, Garst M
Bioorg Med Chem Lett (1995) 5 : 1745 -1750
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.98 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50390 1 9.60
CHEMBL298936 1 8.92
CHEMBL49137 1 8.89
CHEMBL844 BRIMONIDINE 4.0 1 8.62
CHEMBL42139 1 8.51
CHEMBL50769 1 8.28
CHEMBL50430 1 8.11
CHEMBL49284 1 8.02
CHEMBL49395 1 7.39
CHEMBL883 1 7.39
CHEMBL298124 1 6.75
CHEMBL300073 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50390 Ki = 0.25 nM 9.60
CHEMBL298936 Ki = 1.2 nM 8.92
CHEMBL49137 Ki = 1.3 nM 8.89
CHEMBL844 BRIMONIDINE Ki = 2.4 nM 8.62
CHEMBL42139 Ki = 3.1 nM 8.51
CHEMBL50769 Ki = 5.2 nM 8.28
CHEMBL50430 Ki = 7.8 nM 8.11
CHEMBL49284 Ki = 9.6 nM 8.02
CHEMBL49395 Ki = 41.0 nM 7.39
CHEMBL883 Ki = 41.0 nM 7.39
CHEMBL298124 Ki = 180.0 nM 6.75
CHEMBL300073 Ki = 5300.0 nM 5.28