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Assay Detail

CHEMBL643754

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

Binding
Binding affinity was tested on human Alpha-1A adrenergic receptor
33
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological options in the treatment of benign prostatic hyperplasia.
Kenny B, Ballard S, Blagg J, Fox D.
J Med Chem (1997) 40 : 1293 -1315
PubMed 9135028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 8.78 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24778 SILODOSIN 4.0 1 10.40
CHEMBL2051956 DEXNIGULDIPINE 2.0 2 9.80
CHEMBL25554 1 9.80
CHEMBL836 TAMSULOSIN 4.0 3 9.70
CHEMBL2 PRAZOSIN 4.0 1 9.70
CHEMBL267336 1 9.70
CHEMBL5483012 2 9.63
CHEMBL25300 1 9.40
CHEMBL420060 1 9.20
CHEMBL88272 1 9.20
CHEMBL180932 1 9.19
CHEMBL25121 1 9.18
CHEMBL24777 1 9.00
CHEMBL278865 UPIDOSIN 2.0 1 9.00
CHEMBL276932 1 8.90
CHEMBL180561 1 8.73
CHEMBL24981 1 8.60
CHEMBL284103 1 8.50
CHEMBL707 DOXAZOSIN 4.0 1 8.50
CHEMBL282214 1 8.40
CHEMBL279516 INDORAMIN 2.0 1 8.40
CHEMBL284470 1 8.23
CHEMBL709 ALFUZOSIN 4.0 1 8.00
CHEMBL286591 1 7.80
CHEMBL423294 CYCLAZOSIN 1 7.60
CHEMBL25467 1 7.60
CHEMBL611 TERAZOSIN 4.0 1 7.40
CHEMBL27899 1 7.16
CHEMBL543741 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24778 SILODOSIN Ki = 0.03981 nM 10.40
CHEMBL2051956 DEXNIGULDIPINE Ki = 0.1585 nM 9.80
CHEMBL25554 Ki = 0.1585 nM 9.80
CHEMBL836 TAMSULOSIN Ki = 0.1995 nM 9.70
CHEMBL2051956 DEXNIGULDIPINE Ki = 0.1995 nM 9.70
CHEMBL2 PRAZOSIN Ki = 0.1995 nM 9.70
CHEMBL836 TAMSULOSIN Ki = 0.1995 nM 9.70
CHEMBL267336 Ki = 0.1995 nM 9.70
CHEMBL5483012 Ki = 0.2344 nM 9.63
CHEMBL25300 Ki = 0.3981 nM 9.40
CHEMBL420060 Ki = 0.631 nM 9.20
CHEMBL88272 Ki = 0.631 nM 9.20
CHEMBL180932 Ki = 0.6457 nM 9.19
CHEMBL25121 Ki = 0.6607 nM 9.18
CHEMBL278865 UPIDOSIN Ki = 1.0 nM 9.00
CHEMBL24777 Ki = 1.0 nM 9.00
CHEMBL276932 Ki = 1.259 nM 8.90
CHEMBL180561 Ki = 1.862 nM 8.73
CHEMBL5483012 Ki = 1.995 nM 8.70
CHEMBL24981 Ki = 2.512 nM 8.60
CHEMBL284103 Ki = 3.162 nM 8.50
CHEMBL707 DOXAZOSIN Ki = 3.162 nM 8.50
CHEMBL836 TAMSULOSIN Ki = 3.981 nM 8.40
CHEMBL282214 Ki = 3.981 nM 8.40
CHEMBL279516 INDORAMIN Ki = 3.981 nM 8.40
CHEMBL284470 Ki = 5.888 nM 8.23
CHEMBL709 ALFUZOSIN Ki = 10.0 nM 8.00
CHEMBL286591 Ki = 15.85 nM 7.80
CHEMBL25467 Ki = 25.12 nM 7.60
CHEMBL423294 CYCLAZOSIN Ki = 25.12 nM 7.60
CHEMBL611 TERAZOSIN Ki = 39.81 nM 7.40
CHEMBL27899 Ki = 69.18 nM 7.16
CHEMBL543741 Ki = 251.19 nM 6.60