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Assay Detail

CHEMBL1638258

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

Binding
Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells
6
Total Activities
6
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-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.
Sagratini G, Angeli P, Buccioni M, Gulini U, Marucci G, Melchiorre C, Poggesi E, Giardinà D.
Eur J Med Chem (2010) 45 : 5800 -5807
PubMed 20934789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.95 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 10.00
CHEMBL1630938 1 9.61
CHEMBL1630939 1 9.49
CHEMBL1630940 1 9.02
CHEMBL1630942 1 7.81
CHEMBL1630941 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Ki = 0.1 nM 10.00
CHEMBL1630938 Ki = 0.2455 nM 9.61
CHEMBL1630939 Ki = 0.3236 nM 9.49
CHEMBL1630940 Ki = 0.955 nM 9.02
CHEMBL1630942 Ki = 15.49 nM 7.81
CHEMBL1630941 Ki = 17.38 nM 7.76