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Assay Detail

CHEMBL4041236

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

Functional
Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
Nguyen T, German N, Decker AM, Langston TL, Gamage TF, Farquhar CE, Li JX, Wiley JL, Thomas BF, Zhang Y.
J Med Chem (2017) 60 : 7410 -7424
PubMed 28792219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.43 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4105512 1 5.47
CHEMBL4099590 1 5.39
CHEMBL4078811 1 -
CHEMBL4089126 1 -
CHEMBL4067924 1 -
CHEMBL4081259 1 -
CHEMBL4070648 1 -
CHEMBL4097779 1 -
CHEMBL4085745 1 -
CHEMBL4064182 1 -
CHEMBL4064299 1 -
CHEMBL4085844 1 -
CHEMBL4102237 1 -
CHEMBL4077975 1 -
CHEMBL3341861 1 -
CHEMBL4081586 1 -
CHEMBL4071010 1 -
CHEMBL4091847 1 -
CHEMBL4062376 1 -
CHEMBL4084091 1 -
CHEMBL4094495 1 -
CHEMBL4073727 1 -
CHEMBL4092811 1 -
CHEMBL4065139 1 -
CHEMBL4096928 1 -
CHEMBL4078901 1 -
CHEMBL4104660 1 -
CHEMBL4086756 1 -
CHEMBL4067016 1 -
CHEMBL4100542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4105512 IC50 = 3400.0 nM 5.47
CHEMBL4099590 IC50 = 4100.0 nM 5.39
CHEMBL3341861 IC50 > 10000.0 nM -
CHEMBL4093478 IC50 - -
CHEMBL4077975 IC50 > 10000.0 nM -
CHEMBL4102237 IC50 > 10000.0 nM -
CHEMBL4085844 IC50 - -
CHEMBL4064299 IC50 - -
CHEMBL4064182 IC50 - -
CHEMBL4085745 IC50 - -
CHEMBL4097779 IC50 - -
CHEMBL4070648 IC50 - -
CHEMBL4081259 IC50 - -
CHEMBL4067924 IC50 - -
CHEMBL4089126 IC50 - -
CHEMBL4078811 IC50 - -
CHEMBL4096828 IC50 - -
CHEMBL4081586 IC50 - -
CHEMBL4071010 IC50 - -
CHEMBL4091847 IC50 - -
CHEMBL4062376 IC50 - -
CHEMBL4084091 IC50 - -
CHEMBL4094495 IC50 - -
CHEMBL4073727 IC50 - -
CHEMBL4092811 IC50 - -
CHEMBL4065139 IC50 - -
CHEMBL4096928 IC50 - -
CHEMBL4078901 IC50 > 10000.0 nM -
CHEMBL4104660 IC50 - -
CHEMBL4086756 IC50 > 10000.0 nM -
CHEMBL4067016 IC50 - -
CHEMBL4100542 IC50 - -