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Assay Detail

CHEMBL5225731

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

Binding
Antagonist activity at human GPR55 expressed in human U2OS cells assessed as inhibition of LPI-induced receptor activation by measuring beta-arrestin 2 recruitment preincubated for 30 mins followed by LPI addition and measured after 75 mins by microplate reader analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 55 (CHEMBL1075322)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
Figuerola-Asencio L, Morales P, Zhao P, Hurst DP, Sayed SS, Colón KL, Gómez-Cañas M, Fernández-Ruiz J, Croatt MP, Reggio PH, Abood ME, Jagerovic N.
ACS Med Chem Lett (2023) 14 : 18 -25
PubMed 36655130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.22 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1484306 1 6.37
CHEMBL1507657 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1484306 IC50 = 430.0 nM 6.37
CHEMBL1507657 IC50 = 860.0 nM 6.07