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Assay Detail

CHEMBL5504235

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

Binding
Agonist activity at mouse GPR18 expressed in CHO cells assessed as activation by measuring beta-arrestin2 recruitment incubated for 90 mins by luminescence based assay
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

N-arachidonyl glycine receptor (CHEMBL6066225)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Potent, Selective Agonists for the Cannabinoid-like Orphan G Protein-Coupled Receptor GPR18: A Promising Drug Target for Cancer and Immunity.
Mahardhika AB, Załuski M, Schoeder CT, Boshta NM, Schabikowski J, Perri F, Łażewska D, Neumann A, Kremers S, Oneto A, Ressemann A, Latacz G, Namasivayam V, Kieć-Kononowicz K, Müller CE.
J Med Chem (2024) 67 : 9896 -9926
PubMed 38885438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 69 6.45 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557729 1 7.34
CHEMBL5556102 1 7.27
CHEMBL5555231 1 7.24
CHEMBL5523402 1 7.05
CHEMBL5532000 1 6.92
CHEMBL5558124 1 6.91
CHEMBL5556346 1 6.90
CHEMBL5557995 1 6.89
CHEMBL5542965 1 6.82
CHEMBL5555055 1 6.81
CHEMBL5556677 1 6.80
CHEMBL5557839 1 6.79
CHEMBL5557393 1 6.77
CHEMBL5517636 1 6.75
CHEMBL5505829 1 6.71
CHEMBL5558263 1 6.68
CHEMBL5549936 1 6.67
CHEMBL5512594 1 6.66
CHEMBL5556049 1 6.64
CHEMBL5559512 1 6.62
CHEMBL5532256 1 6.61
CHEMBL5523442 1 6.61
CHEMBL5555914 1 6.60
CHEMBL5557780 1 6.55
CHEMBL5556617 1 6.55
CHEMBL5556551 1 6.54
CHEMBL5559109 1 6.54
CHEMBL5557906 1 6.53
CHEMBL5517653 1 6.52
CHEMBL5542310 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557729 EC50 = 46.0 nM 7.34
CHEMBL5556102 EC50 = 54.0 nM 7.27
CHEMBL5555231 EC50 = 58.0 nM 7.24
CHEMBL5523402 EC50 = 90.0 nM 7.05
CHEMBL5532000 EC50 = 121.0 nM 6.92
CHEMBL5558124 EC50 = 124.0 nM 6.91
CHEMBL5556346 EC50 = 127.0 nM 6.90
CHEMBL5557995 EC50 = 128.0 nM 6.89
CHEMBL5542965 EC50 = 150.0 nM 6.82
CHEMBL5555055 EC50 = 156.0 nM 6.81
CHEMBL5556677 EC50 = 157.0 nM 6.80
CHEMBL5557839 EC50 = 161.0 nM 6.79
CHEMBL5557393 EC50 = 171.0 nM 6.77
CHEMBL5517636 EC50 = 180.0 nM 6.75
CHEMBL5505829 EC50 = 194.0 nM 6.71
CHEMBL5558263 EC50 = 207.0 nM 6.68
CHEMBL5549936 EC50 = 216.0 nM 6.67
CHEMBL5512594 EC50 = 220.0 nM 6.66
CHEMBL5556049 EC50 = 230.0 nM 6.64
CHEMBL5559512 EC50 = 241.0 nM 6.62
CHEMBL5532256 EC50 = 244.0 nM 6.61
CHEMBL5523442 EC50 = 245.0 nM 6.61
CHEMBL5555914 EC50 = 251.0 nM 6.60
CHEMBL5557780 EC50 = 281.0 nM 6.55
CHEMBL5556617 EC50 = 280.0 nM 6.55
CHEMBL5556551 EC50 = 290.0 nM 6.54
CHEMBL5559109 EC50 = 288.0 nM 6.54
CHEMBL5557906 EC50 = 297.0 nM 6.53
CHEMBL5517653 EC50 = 299.0 nM 6.52
CHEMBL5542310 EC50 = 301.0 nM 6.52
CHEMBL5523497 EC50 = 318.0 nM 6.50
CHEMBL5558536 EC50 = 334.0 nM 6.48
CHEMBL5505756 EC50 = 371.0 nM 6.43
CHEMBL5505898 EC50 = 379.0 nM 6.42
CHEMBL5517700 EC50 = 379.0 nM 6.42
CHEMBL5558192 EC50 = 393.0 nM 6.41
CHEMBL5556254 EC50 = 398.0 nM 6.40
CHEMBL5558126 EC50 = 444.0 nM 6.35
CHEMBL5558903 EC50 = 447.0 nM 6.35
CHEMBL5557185 EC50 = 488.0 nM 6.31
CHEMBL5527882 EC50 = 559.0 nM 6.25
CHEMBL4758188 EC50 = 582.0 nM 6.24
CHEMBL5523663 EC50 = 711.0 nM 6.15
CHEMBL5556616 EC50 = 981.0 nM 6.01
CHEMBL5555175 EC50 = 1200.0 nM 5.92
CHEMBL5558336 EC50 = 1270.0 nM 5.90
CHEMBL5556620 EC50 = 1300.0 nM 5.89
CHEMBL239232 EC50 = 1780.0 nM 5.75
CHEMBL5505788 EC50 = 2640.0 nM 5.58
CHEMBL5557962 EC50 = 2970.0 nM 5.53