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Assay Detail

CHEMBL5504232

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Functional
Agonist activity at human GPR18 expressed in CHO cells assessed as activation by measuring beta-arrestin2 recruitment incubated for 90 mins by luminescence based assay
ChEMBL ↗
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

N-arachidonyl glycine receptor (CHEMBL2384898) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 74 6.63 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5517636 — — 1 8.00
CHEMBL5556102 — — 1 7.72
CHEMBL5557729 — — 1 7.62
CHEMBL5556617 — — 1 7.38
CHEMBL5558124 — — 1 7.27
CHEMBL5556677 — — 1 7.22
CHEMBL5532256 — — 1 7.19
CHEMBL5512594 — — 1 7.15
CHEMBL5555231 — — 1 7.14
CHEMBL5523402 — — 1 7.13
CHEMBL5532000 — — 1 7.10
CHEMBL5557906 — — 1 7.02
CHEMBL5556346 — — 1 6.99
CHEMBL5558903 — — 1 6.96
CHEMBL5542310 — — 1 6.94
CHEMBL5556049 — — 1 6.92
CHEMBL5549936 — — 1 6.87
CHEMBL5557393 — — 1 6.86
CHEMBL5557995 — — 1 6.86
CHEMBL5557839 — — 1 6.85
CHEMBL5505829 — — 1 6.83
CHEMBL5558263 — — 1 6.82
CHEMBL5523442 — — 1 6.78
CHEMBL5505898 — — 1 6.77
CHEMBL5555055 — — 1 6.72
CHEMBL5517700 — — 1 6.72
CHEMBL5517653 — — 1 6.71
CHEMBL5555914 — — 1 6.71
CHEMBL5556551 — — 1 6.69
CHEMBL5557780 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5517636 — EC50 = 10.0 nM 8.00
CHEMBL5556102 — EC50 = 19.0 nM 7.72
CHEMBL5557729 — EC50 = 24.0 nM 7.62
CHEMBL5556617 — EC50 = 42.0 nM 7.38
CHEMBL5558124 — EC50 = 54.0 nM 7.27
CHEMBL5556677 — EC50 = 60.0 nM 7.22
CHEMBL5532256 — EC50 = 64.0 nM 7.19
CHEMBL5512594 — EC50 = 71.0 nM 7.15
CHEMBL5555231 — EC50 = 72.0 nM 7.14
CHEMBL5523402 — EC50 = 74.0 nM 7.13
CHEMBL5532000 — EC50 = 80.0 nM 7.10
CHEMBL5557906 — EC50 = 95.0 nM 7.02
CHEMBL5556346 — EC50 = 102.0 nM 6.99
CHEMBL5558903 — EC50 = 111.0 nM 6.96
CHEMBL5542310 — EC50 = 115.0 nM 6.94
CHEMBL5556049 — EC50 = 120.0 nM 6.92
CHEMBL5549936 — EC50 = 136.0 nM 6.87
CHEMBL5557393 — EC50 = 138.0 nM 6.86
CHEMBL5557995 — EC50 = 137.0 nM 6.86
CHEMBL5557839 — EC50 = 142.0 nM 6.85
CHEMBL5505829 — EC50 = 149.0 nM 6.83
CHEMBL5558263 — EC50 = 151.0 nM 6.82
CHEMBL5523442 — EC50 = 166.0 nM 6.78
CHEMBL5505898 — EC50 = 169.0 nM 6.77
CHEMBL5517700 — EC50 = 190.0 nM 6.72
CHEMBL5555055 — EC50 = 189.0 nM 6.72
CHEMBL5517653 — EC50 = 196.0 nM 6.71
CHEMBL5555914 — EC50 = 193.0 nM 6.71
CHEMBL5556551 — EC50 = 206.0 nM 6.69
CHEMBL5557780 — EC50 = 218.0 nM 6.66
CHEMBL5558536 — EC50 = 229.0 nM 6.64
CHEMBL5523497 — EC50 = 247.0 nM 6.61
CHEMBL5505756 — EC50 = 254.0 nM 6.59
CHEMBL5559512 — EC50 = 261.0 nM 6.58
CHEMBL5556254 — EC50 = 351.0 nM 6.46
CHEMBL5527882 — EC50 = 347.0 nM 6.46
CHEMBL5542965 — EC50 = 352.0 nM 6.45
CHEMBL5558126 — EC50 = 417.0 nM 6.38
CHEMBL5559109 — EC50 = 442.0 nM 6.36
CHEMBL4758188 — EC50 = 454.0 nM 6.34
CHEMBL5557185 — EC50 = 469.0 nM 6.33
CHEMBL5523663 — EC50 = 486.0 nM 6.31
CHEMBL239232 — EC50 = 562.0 nM 6.25
CHEMBL5556620 — EC50 = 584.0 nM 6.23
CHEMBL5557962 — EC50 = 902.0 nM 6.04
CHEMBL5556616 — EC50 = 1220.0 nM 5.91
CHEMBL5505788 — EC50 = 1390.0 nM 5.86
CHEMBL5558336 — EC50 = 1410.0 nM 5.85
CHEMBL5555175 — EC50 = 1630.0 nM 5.79
CHEMBL465 DRONABINOL EC50 = 3370.0 nM 5.47