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Assay Detail

CHEMBL3381315

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

Binding
Displacement of [3H]prazosin from human recombinant alpha1D adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
27
Total Activities
27
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

Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands at α<alpha>1 and 5-HT1A receptors.
Franchini S, Battisti UM, Baraldi A, Prandi A, Fossa P, Cichero E, Tait A, Sorbi C, Marucci G, Cilia A, Pirona L, Brasili L.
Eur J Med Chem (2014) 87 : 248 -266
PubMed 25261823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.72 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342871 1 9.04
CHEMBL3342853 1 8.33
CHEMBL3342870 1 8.24
CHEMBL3342868 1 8.15
CHEMBL3342857 1 8.09
CHEMBL3342872 1 8.01
CHEMBL3342867 1 7.97
CHEMBL3342860 1 7.96
CHEMBL3342866 1 7.91
CHEMBL3342874 1 7.88
CHEMBL3342852 1 7.83
CHEMBL3342875 1 7.72
CHEMBL3342859 1 7.69
CHEMBL3342858 1 7.64
CHEMBL3342873 1 7.63
CHEMBL3341769 1 7.60
CHEMBL3342869 1 7.58
CHEMBL3342863 1 7.57
CHEMBL3342861 1 7.55
CHEMBL3342876 1 7.45
CHEMBL3342856 1 7.43
CHEMBL3342862 1 7.40
CHEMBL3342854 1 7.37
CHEMBL3342855 1 7.29
CHEMBL3342864 1 7.05
CHEMBL3342865 1 6.38
CHEMBL2234448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342871 Ki = 0.912 nM 9.04
CHEMBL3342853 Ki = 4.677 nM 8.33
CHEMBL3342870 Ki = 5.754 nM 8.24
CHEMBL3342868 Ki = 7.079 nM 8.15
CHEMBL3342857 Ki = 8.128 nM 8.09
CHEMBL3342872 Ki = 9.772 nM 8.01
CHEMBL3342867 Ki = 10.72 nM 7.97
CHEMBL3342860 Ki = 10.96 nM 7.96
CHEMBL3342866 Ki = 12.3 nM 7.91
CHEMBL3342874 Ki = 13.18 nM 7.88
CHEMBL3342852 Ki = 14.79 nM 7.83
CHEMBL3342875 Ki = 19.05 nM 7.72
CHEMBL3342859 Ki = 20.42 nM 7.69
CHEMBL3342858 Ki = 22.91 nM 7.64
CHEMBL3342873 Ki = 23.44 nM 7.63
CHEMBL3341769 Ki = 25.12 nM 7.60
CHEMBL3342869 Ki = 26.3 nM 7.58
CHEMBL3342863 Ki = 26.92 nM 7.57
CHEMBL3342861 Ki = 28.18 nM 7.55
CHEMBL3342876 Ki = 35.48 nM 7.45
CHEMBL3342856 Ki = 37.15 nM 7.43
CHEMBL3342862 Ki = 39.81 nM 7.40
CHEMBL3342854 Ki = 42.66 nM 7.37
CHEMBL3342855 Ki = 51.29 nM 7.29
CHEMBL3342864 Ki = 89.13 nM 7.05
CHEMBL3342865 Ki = 416.87 nM 6.38
CHEMBL2234448 Ki > 1000.0 nM -