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Assay Detail

CHEMBL917772

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

Binding
Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells
32
Total Activities
32
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 Expert

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.
Muccioli GG, Wouters J, Scriba GK, Poppitz W, Poupaert JH, Lambert DM.
J Med Chem (2005) 48 : 7486 -7490
PubMed 16279809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.03 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111 RIMONABANT 4.0 1 8.27
CHEMBL334533 DEXANABINOL 3.0 1 7.72
CHEMBL427241 1 6.30
CHEMBL224627 1 6.19
CHEMBL388398 1 6.12
CHEMBL224113 1 5.96
CHEMBL436309 1 5.90
CHEMBL224697 1 5.82
CHEMBL224904 1 5.75
CHEMBL224905 1 5.72
CHEMBL225003 1 5.56
CHEMBL224748 1 5.54
CHEMBL391003 1 5.54
CHEMBL388399 1 5.46
CHEMBL188 WIN-552122 1 5.42
CHEMBL375286 1 5.15
CHEMBL370626 1 -
CHEMBL224575 1 -
CHEMBL224626 1 -
CHEMBL224052 1 -
CHEMBL224337 1 -
CHEMBL224388 1 -
CHEMBL225361 1 -
CHEMBL225568 1 -
CHEMBL427088 1 -
CHEMBL224954 1 -
CHEMBL225414 1 -
CHEMBL225379 1 -
CHEMBL199555 1 -
CHEMBL376129 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111 RIMONABANT Ki = 5.4 nM 8.27
CHEMBL334533 DEXANABINOL Ki = 19.0 nM 7.72
CHEMBL427241 Ki = 500.0 nM 6.30
CHEMBL224627 Ki = 650.0 nM 6.19
CHEMBL388398 Ki = 750.0 nM 6.12
CHEMBL224113 Ki = 1100.0 nM 5.96
CHEMBL436309 Ki = 1250.0 nM 5.90
CHEMBL224697 Ki = 1500.0 nM 5.82
CHEMBL224904 Ki = 1800.0 nM 5.75
CHEMBL224905 Ki = 1900.0 nM 5.72
CHEMBL225003 Ki = 2750.0 nM 5.56
CHEMBL391003 Ki = 2900.0 nM 5.54
CHEMBL224748 Ki = 2900.0 nM 5.54
CHEMBL388399 Ki = 3450.0 nM 5.46
CHEMBL188 WIN-552122 Ki = 3800.0 nM 5.42
CHEMBL375286 Ki = 7050.0 nM 5.15
CHEMBL224515 Ki - -
CHEMBL374160 Ki - -
CHEMBL376129 Ki - -
CHEMBL199555 Ki - -
CHEMBL225379 Ki - -
CHEMBL225414 Ki - -
CHEMBL224954 Ki - -
CHEMBL427088 Ki - -
CHEMBL225568 Ki - -
CHEMBL225361 Ki - -
CHEMBL224388 Ki - -
CHEMBL224337 Ki - -
CHEMBL224052 Ki - -
CHEMBL224626 Ki - -
CHEMBL224575 Ki - -
CHEMBL370626 Ki - -