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Assay Detail

CHEMBL4670130

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

Binding
Antagonist activity at 5HT2C receptor (unknown origin) by radioligand binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT receptor antagonist scaffold.
Kim M,Truss M,Pagare PP,Essandoh MA,Zhang Y,Williams DA
Bioorg Med Chem Lett (2020) 30 : 127511 -127511
PubMed 32853682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.70 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4795598 1 6.10
CHEMBL4755344 1 5.70
CHEMBL4763861 1 5.50
CHEMBL4741776 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4795598 Ki = 794.33 nM 6.10
CHEMBL4755344 Ki = 1995.26 nM 5.70
CHEMBL4763861 Ki = 3162.28 nM 5.50
CHEMBL4741776 Ki = 3162.28 nM 5.50