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Assay Detail

CHEMBL3381316

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HeLa 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 HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
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 7.37 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2234448 1 8.29
CHEMBL3342858 1 8.05
CHEMBL3342852 1 8.03
CHEMBL3342853 1 7.84
CHEMBL3342857 1 7.80
CHEMBL3342862 1 7.69
CHEMBL3342870 1 7.61
CHEMBL3342867 1 7.57
CHEMBL3342874 1 7.48
CHEMBL3342863 1 7.44
CHEMBL3342868 1 7.43
CHEMBL3342861 1 7.37
CHEMBL3342871 1 7.36
CHEMBL3341769 1 7.33
CHEMBL3342860 1 7.30
CHEMBL3342866 1 7.28
CHEMBL3342859 1 7.23
CHEMBL3342872 1 7.22
CHEMBL3342864 1 7.19
CHEMBL3342869 1 7.16
CHEMBL3342875 1 7.10
CHEMBL3342855 1 7.09
CHEMBL3342876 1 7.06
CHEMBL3342854 1 6.93
CHEMBL3342873 1 6.84
CHEMBL3342856 1 6.80
CHEMBL3342865 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2234448 Ki = 5.129 nM 8.29
CHEMBL3342858 Ki = 8.913 nM 8.05
CHEMBL3342852 Ki = 9.333 nM 8.03
CHEMBL3342853 Ki = 14.45 nM 7.84
CHEMBL3342857 Ki = 15.85 nM 7.80
CHEMBL3342862 Ki = 20.42 nM 7.69
CHEMBL3342870 Ki = 24.55 nM 7.61
CHEMBL3342867 Ki = 26.92 nM 7.57
CHEMBL3342874 Ki = 33.11 nM 7.48
CHEMBL3342863 Ki = 36.31 nM 7.44
CHEMBL3342868 Ki = 37.15 nM 7.43
CHEMBL3342861 Ki = 42.66 nM 7.37
CHEMBL3342871 Ki = 43.65 nM 7.36
CHEMBL3341769 Ki = 46.77 nM 7.33
CHEMBL3342860 Ki = 50.12 nM 7.30
CHEMBL3342866 Ki = 52.48 nM 7.28
CHEMBL3342859 Ki = 58.88 nM 7.23
CHEMBL3342872 Ki = 60.26 nM 7.22
CHEMBL3342864 Ki = 64.57 nM 7.19
CHEMBL3342869 Ki = 69.18 nM 7.16
CHEMBL3342875 Ki = 79.43 nM 7.10
CHEMBL3342855 Ki = 81.28 nM 7.09
CHEMBL3342876 Ki = 87.1 nM 7.06
CHEMBL3342854 Ki = 117.49 nM 6.93
CHEMBL3342873 Ki = 144.54 nM 6.84
CHEMBL3342856 Ki = 158.49 nM 6.80
CHEMBL3342865 Ki = 323.59 nM 6.49