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Assay Detail

CHEMBL2445944

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

Binding
Displacement of [3H]GR65630 from human recombinant 5HT3 receptor expressed in HEKT cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
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 9 5.74 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2058426 1 6.23
CHEMBL2058419 1 6.18
CHEMBL1170237 1 6.00
CHEMBL2058420 1 5.91
CHEMBL512332 METHYLAPLYSINOPSIN 1 5.82
CHEMBL2058427 1 5.58
CHEMBL404232 APLYSINOPSIN 1 5.52
CHEMBL2058415 1 5.23
CHEMBL2058416 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2058426 Ki = 591.0 nM 6.23
CHEMBL2058419 Ki = 656.0 nM 6.18
CHEMBL1170237 Ki = 1000.0 nM 6.00
CHEMBL2058420 Ki = 1223.0 nM 5.91
CHEMBL512332 METHYLAPLYSINOPSIN Ki = 1511.0 nM 5.82
CHEMBL2058427 Ki = 2624.0 nM 5.58
CHEMBL404232 APLYSINOPSIN Ki = 3029.0 nM 5.52
CHEMBL2058415 Ki = 5916.0 nM 5.23
CHEMBL2058416 Ki = 6178.0 nM 5.21