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Assay Detail

CHEMBL4123783

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

Binding
Displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
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

Chiral analogues of (+)-cyclazosin as potent α1B-adrenoceptor selective antagonist.
Sagratini G, Buccioni M, Marucci G, Poggesi E, Skorski M, Costanzi S, Giardinà D.
Bioorg Med Chem (2018) 26 : 3502 -3513
PubMed 29784274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 9.39 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342062 1 10.15
CHEMBL4126860 1 9.89
CHEMBL423294 CYCLAZOSIN 1 9.87
CHEMBL4129291 1 9.82
CHEMBL4128084 1 9.72
CHEMBL4127483 1 9.52
CHEMBL4125981 1 9.42
CHEMBL4129461 1 9.13
CHEMBL4128460 1 9.11
CHEMBL4127078 1 9.04
CHEMBL4125846 1 8.93
CHEMBL4128311 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342062 Ki = 0.07079 nM 10.15
CHEMBL4126860 Ki = 0.1288 nM 9.89
CHEMBL423294 CYCLAZOSIN Ki = 0.1349 nM 9.87
CHEMBL4129291 Ki = 0.1514 nM 9.82
CHEMBL4128084 Ki = 0.1905 nM 9.72
CHEMBL4127483 Ki = 0.302 nM 9.52
CHEMBL4125981 Ki = 0.3802 nM 9.42
CHEMBL4129461 Ki = 0.7413 nM 9.13
CHEMBL4128460 Ki = 0.7762 nM 9.11
CHEMBL4127078 Ki = 0.912 nM 9.04
CHEMBL4125846 Ki = 1.175 nM 8.93
CHEMBL4128311 Ki = 9.12 nM 8.04