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Assay Detail

CHEMBL4139219

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

Binding
Displacement of [3H]prazosin from human alpha1B adrenoceptor expressed in CHO cell membranes after 30 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinazoline based α1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines.
Maestri V, Tarozzi A, Simoni E, Cilia A, Poggesi E, Naldi M, Nicolini B, Pruccoli L, Rosini M, Minarini A.
Eur J Med Chem (2017) 136 : 259 -269
PubMed 28499171 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.96 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161165 1 9.55
CHEMBL2 PRAZOSIN 4.0 1 9.39
CHEMBL4163587 1 9.28
CHEMBL707 DOXAZOSIN 4.0 1 9.20
CHEMBL4160032 1 8.13
CHEMBL4171491 1 7.60
CHEMBL4171710 1 7.37
CHEMBL4159468 1 7.33
CHEMBL4163810 1 7.26
CHEMBL4170675 1 7.20
CHEMBL4174168 1 6.75
CHEMBL4167693 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161165 Ki = 0.2818 nM 9.55
CHEMBL2 PRAZOSIN Ki = 0.4074 nM 9.39
CHEMBL4163587 Ki = 0.5248 nM 9.28
CHEMBL707 DOXAZOSIN Ki = 0.631 nM 9.20
CHEMBL4160032 Ki = 7.413 nM 8.13
CHEMBL4171491 Ki = 25.12 nM 7.60
CHEMBL4171710 Ki = 42.66 nM 7.37
CHEMBL4159468 Ki = 46.77 nM 7.33
CHEMBL4163810 Ki = 54.95 nM 7.26
CHEMBL4170675 Ki = 63.1 nM 7.20
CHEMBL4174168 Ki = 177.83 nM 6.75
CHEMBL4167693 Ki = 316.23 nM 6.50