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Assay Detail

CHEMBL5225729

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

Binding
Antagonist activity at beta-galactosidase fused human GPR55 expressed in CHO cells assessed as inhibition of LPI-induced receptor activation by measuring beta-arrestin 2 recruitment incubated for 90 mins by PathHunter chemiluminescence based assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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 13 5.46 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5273189 1 6.55
CHEMBL5273001 1 6.17
CHEMBL1402920 1 5.70
CHEMBL5278819 1 5.67
CHEMBL5281110 1 5.64
CHEMBL5282587 1 5.56
CHEMBL5271818 1 5.52
CHEMBL5275607 1 5.47
CHEMBL5267293 1 5.14
CHEMBL5278170 1 5.10
CHEMBL5283686 1 5.02
CHEMBL5267388 1 4.93
CHEMBL5281025 1 4.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5273189 IC50 = 280.0 nM 6.55
CHEMBL5273001 IC50 = 680.0 nM 6.17
CHEMBL1402920 IC50 = 2020.0 nM 5.70
CHEMBL5278819 IC50 = 2140.0 nM 5.67
CHEMBL5281110 IC50 = 2300.0 nM 5.64
CHEMBL5282587 IC50 = 2780.0 nM 5.56
CHEMBL5271818 IC50 = 3000.0 nM 5.52
CHEMBL5275607 IC50 = 3350.0 nM 5.47
CHEMBL5267293 IC50 = 7160.0 nM 5.14
CHEMBL5278170 IC50 = 8000.0 nM 5.10
CHEMBL5283686 IC50 = 9490.0 nM 5.02
CHEMBL5267388 IC50 = 11700.0 nM 4.93
CHEMBL5281025 IC50 = 29300.0 nM 4.53