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Assay Detail

CHEMBL2445941

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

Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.
Lewellyn K, Bialonska D, Loria MJ, White SW, Sufka KJ, Zjawiony JK.
Bioorg Med Chem (2013) 21 : 7083 -7090
PubMed 24084296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.61 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442272 1 6.13
CHEMBL2058704 1 6.07
CHEMBL2058415 1 5.85
CHEMBL2442274 1 5.85
CHEMBL512332 METHYLAPLYSINOPSIN 1 5.76
CHEMBL2058418 1 5.64
CHEMBL2058703 1 5.43
CHEMBL2058429 1 5.14
CHEMBL2058426 1 5.12
CHEMBL404232 APLYSINOPSIN 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442272 Ki = 742.0 nM 6.13
CHEMBL2058704 Ki = 860.0 nM 6.07
CHEMBL2058415 Ki = 1409.0 nM 5.85
CHEMBL2442274 Ki = 1405.0 nM 5.85
CHEMBL512332 METHYLAPLYSINOPSIN Ki = 1716.0 nM 5.76
CHEMBL2058418 Ki = 2306.0 nM 5.64
CHEMBL2058703 Ki = 3733.0 nM 5.43
CHEMBL2058429 Ki = 7300.0 nM 5.14
CHEMBL2058426 Ki = 7523.0 nM 5.12
CHEMBL404232 APLYSINOPSIN Ki = 8768.0 nM 5.06