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Assay Detail

CHEMBL643228

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

Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
11
Total Activities
11
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

Pharmacological evaluation of UK-14,304 analogs at cloned human adrenergic receptors
Jeon YT, Luo C, Forray C, Vaysse PJ, Branchek TA, Gluchowski C
Bioorg Med Chem Lett (1995) 5 : 2255 -2258
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.69 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74283 1 8.19
CHEMBL844 BRIMONIDINE 4.0 1 8.17
CHEMBL70676 1 8.17
CHEMBL49137 1 8.14
CHEMBL72753 1 7.43
CHEMBL72147 1 7.13
CHEMBL49395 1 6.51
CHEMBL72995 1 5.42
CHEMBL73392 1 4.99
CHEMBL74342 1 4.83
CHEMBL73164 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74283 Ki = 6.457 nM 8.19
CHEMBL844 BRIMONIDINE Ki = 6.761 nM 8.17
CHEMBL70676 Ki = 6.761 nM 8.17
CHEMBL49137 Ki = 7.244 nM 8.14
CHEMBL72753 Ki = 37.15 nM 7.43
CHEMBL72147 Ki = 74.13 nM 7.13
CHEMBL49395 Ki = 309.03 nM 6.51
CHEMBL72995 Ki = 3801.89 nM 5.42
CHEMBL73392 Ki = 10232.93 nM 4.99
CHEMBL74342 Ki = 14791.08 nM 4.83
CHEMBL73164 Ki = 26302.68 nM 4.58