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Assay Detail

CHEMBL643530

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

Binding
Binding affinity for Alpha-1 adrenergic receptor of human cerebral cortex membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
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 5.51 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50390 1 6.89
CHEMBL298936 1 6.33
CHEMBL49137 1 5.85
CHEMBL50769 1 5.82
CHEMBL844 BRIMONIDINE 4.0 1 5.72
CHEMBL42139 1 5.62
CHEMBL50430 1 5.60
CHEMBL49284 1 5.05
CHEMBL300073 1 5.00
CHEMBL49395 1 4.96
CHEMBL883 1 4.77
CHEMBL298124 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50390 Ki = 130.0 nM 6.89
CHEMBL298936 Ki = 470.0 nM 6.33
CHEMBL49137 Ki = 1400.0 nM 5.85
CHEMBL50769 Ki = 1500.0 nM 5.82
CHEMBL844 BRIMONIDINE Ki = 1900.0 nM 5.72
CHEMBL42139 Ki = 2400.0 nM 5.62
CHEMBL50430 Ki = 2500.0 nM 5.60
CHEMBL49284 Ki = 8900.0 nM 5.05
CHEMBL300073 Ki = 10000.0 nM 5.00
CHEMBL49395 Ki = 11000.0 nM 4.96
CHEMBL883 Ki = 17000.0 nM 4.77
CHEMBL298124 Ki = 30000.0 nM 4.52