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Assay Detail

CHEMBL5161385

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

Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of a Pyrimidinone Series for Selective Inhibition of Ca<sup>2+</sup>/Calmodulin-Stimulated Adenylyl Cyclase 1 Activity for the Treatment of Chronic Pain.
Scott JA, Soto-Velasquez M, Hayes MP, LaVigne JE, Miller HR, Kaur J, Ejendal KFK, Watts VJ, Flaherty DP.
J Med Chem (2022) 65 : 4667 -4686
PubMed 35271288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.38 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187824 1 6.38
CHEMBL5188949 1 6.38
CHEMBL5202029 1 6.38
CHEMBL5182403 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187824 IC50 = 420.0 nM 6.38
CHEMBL5188949 IC50 = 420.0 nM 6.38
CHEMBL5202029 IC50 = 420.0 nM 6.38
CHEMBL5182403 IC50 = 420.0 nM 6.38