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Assay Detail

CHEMBL3777632

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

Binding
Antagonist activity at HA-epitope tagged GRP55E expressed with GFP-tagged beta-arr2 in human U2OS cells assessed as LPI-stimulated redistribution of beta-arr2 preincubated for 15 mins by beta-arrestin translocation assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones.
Meza-Aviña ME, Lingerfelt MA, Console-Bram LM, Gamage TF, Sharir H, Gettys KE, Hurst DP, Kotsikorou E, Shore DM, Caron MG, Rao N, Barak LS, Abood ME, Reggio PH, Croatt MP.
Bioorg Med Chem Lett (2016) 26 : 1827 -1830
PubMed 26916440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.26 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1310336 1 6.66
CHEMBL1402920 1 6.16
CHEMBL1366039 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1310336 IC50 = 220.0 nM 6.66
CHEMBL1402920 IC50 = 700.0 nM 6.16
CHEMBL1366039 IC50 = 1100.0 nM 5.96