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Assay Detail

CHEMBL5161380

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Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
4
Total Activities
4
Compounds Tested
2
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 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
Ki 2 5.97 6.05
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188949 1 6.05
CHEMBL5187824 1 5.89
CHEMBL5202029 1 -
CHEMBL5182403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188949 Ki = 900.0 nM 6.05
CHEMBL5187824 Ki = 1300.0 nM 5.89
CHEMBL5202029 Inhibition = 49.0 % -
CHEMBL5182403 Inhibition = 32.0 % -