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Assay Detail

CHEMBL643751

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

Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
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-1A adrenergic receptor (CHEMBL229)
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 5.21 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70676 1 6.01
CHEMBL74283 1 5.95
CHEMBL49137 1 5.83
CHEMBL844 BRIMONIDINE 4.0 1 5.55
CHEMBL72753 1 5.29
CHEMBL74342 1 4.85
CHEMBL49395 1 4.74
CHEMBL73392 1 4.67
CHEMBL73164 1 4.04
CHEMBL72995 1 -
CHEMBL72147 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70676 Ki = 977.24 nM 6.01
CHEMBL74283 Ki = 1122.02 nM 5.95
CHEMBL49137 Ki = 1479.11 nM 5.83
CHEMBL844 BRIMONIDINE Ki = 2818.38 nM 5.55
CHEMBL72753 Ki = 5128.61 nM 5.29
CHEMBL74342 Ki = 14125.38 nM 4.85
CHEMBL49395 Ki = 18197.01 nM 4.74
CHEMBL73392 Ki = 21379.62 nM 4.67
CHEMBL73164 Ki = 91201.08 nM 4.04
CHEMBL72995 Ki < 100000.0 nM -
CHEMBL72147 Ki < 100000.0 nM -