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Assay Detail

CHEMBL4123782

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

Binding
Displacement of [3H]prazosin from human alpha1A 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-1A adrenergic receptor (CHEMBL229)
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 8.25 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128084 1 9.30
CHEMBL342062 1 9.23
CHEMBL4129291 1 9.06
CHEMBL4126860 1 8.73
CHEMBL4125981 1 8.26
CHEMBL4127078 1 8.24
CHEMBL4128460 1 8.18
CHEMBL4129461 1 8.04
CHEMBL423294 CYCLAZOSIN 1 7.91
CHEMBL4125846 1 7.77
CHEMBL4127483 1 7.65
CHEMBL4128311 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128084 Ki = 0.5012 nM 9.30
CHEMBL342062 Ki = 0.5888 nM 9.23
CHEMBL4129291 Ki = 0.871 nM 9.06
CHEMBL4126860 Ki = 1.862 nM 8.73
CHEMBL4125981 Ki = 5.495 nM 8.26
CHEMBL4127078 Ki = 5.754 nM 8.24
CHEMBL4128460 Ki = 6.607 nM 8.18
CHEMBL4129461 Ki = 9.12 nM 8.04
CHEMBL423294 CYCLAZOSIN Ki = 12.3 nM 7.91
CHEMBL4125846 Ki = 16.98 nM 7.77
CHEMBL4127483 Ki = 22.39 nM 7.65
CHEMBL4128311 Ki = 223.87 nM 6.65