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Assay Detail

CHEMBL2388875

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

Binding
Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay
35
Total Activities
35
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

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

Publication

Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold.
Rempel V, Volz N, Gläser F, Nieger M, Bräse S, Müller CE.
J Med Chem (2013) 56 : 4798 -4810
PubMed 23679955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 4.99 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 5.22
CHEMBL2177264 1 5.09
CHEMBL111 RIMONABANT 4.0 1 5.00
CHEMBL2387530 1 5.00
CHEMBL2387744 1 4.95
CHEMBL2181542 1 4.90
CHEMBL2181540 1 4.80
CHEMBL2387538 1 -
CHEMBL2177263 1 -
CHEMBL2387539 1 -
CHEMBL2177257 1 -
CHEMBL2181546 1 -
CHEMBL2177250 1 -
CHEMBL2177253 1 -
CHEMBL2177254 1 -
CHEMBL2177259 1 -
CHEMBL2177260 1 -
CHEMBL2387532 1 -
CHEMBL2387537 1 -
CHEMBL2387536 1 -
CHEMBL2387535 1 -
CHEMBL2387534 1 -
CHEMBL2387533 1 -
CHEMBL470199 1 -
CHEMBL2181551 1 -
CHEMBL506746 1 -
CHEMBL2177249 1 -
CHEMBL2387743 1 -
CHEMBL2181549 1 -
CHEMBL470224 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 IC50 = 5990.0 nM 5.22
CHEMBL2177264 IC50 = 8100.0 nM 5.09
CHEMBL111 RIMONABANT IC50 = 10100.0 nM 5.00
CHEMBL2387530 IC50 = 10000.0 nM 5.00
CHEMBL2387744 IC50 = 11300.0 nM 4.95
CHEMBL2181542 IC50 = 12500.0 nM 4.90
CHEMBL2181540 IC50 = 15900.0 nM 4.80
CHEMBL2177257 IC50 > 10000.0 nM -
CHEMBL2181545 IC50 > 10000.0 nM -
CHEMBL2181546 IC50 >= 10000.0 nM -
CHEMBL2177250 IC50 > 10000.0 nM -
CHEMBL2177253 IC50 > 10000.0 nM -
CHEMBL2177254 IC50 > 10000.0 nM -
CHEMBL2177259 IC50 > 10000.0 nM -
CHEMBL2177260 IC50 > 10000.0 nM -
CHEMBL2387532 IC50 > 10000.0 nM -
CHEMBL2177263 IC50 > 10000.0 nM -
CHEMBL2181539 IC50 > 10000.0 nM -
CHEMBL2181541 IC50 > 10000.0 nM -
CHEMBL2181543 IC50 > 10000.0 nM -
CHEMBL2181544 IC50 >= 10000.0 nM -
CHEMBL2387539 IC50 > 10000.0 nM -
CHEMBL2387538 IC50 > 10000.0 nM -
CHEMBL2387537 IC50 >= 10000.0 nM -
CHEMBL2387536 IC50 > 10000.0 nM -
CHEMBL2387535 IC50 > 10000.0 nM -
CHEMBL2387534 IC50 >= 10000.0 nM -
CHEMBL2387533 IC50 > 10000.0 nM -
CHEMBL470199 IC50 > 10000.0 nM -
CHEMBL2181551 IC50 > 10000.0 nM -
CHEMBL506746 IC50 > 10000.0 nM -
CHEMBL2177249 IC50 > 10000.0 nM -
CHEMBL2387743 IC50 > 10000.0 nM -
CHEMBL2181549 IC50 > 10000.0 nM -
CHEMBL470224 IC50 > 10000.0 nM -