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Assay Detail

CHEMBL2388872

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

Binding
Displacement of [3H]-CP55,940 from human CB1 receptor transfected in CHOK1 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
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
Ki 19 5.74 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL465 DRONABINOL 4.0 1 8.41
CHEMBL2387530 1 6.21
CHEMBL2387533 1 5.44
CHEMBL2387538 1 5.11
CHEMBL2181541 1 5.00
CHEMBL2387536 1 5.00
CHEMBL2387532 1 4.99
CHEMBL2181545 1 -
CHEMBL506746 1 -
CHEMBL470224 1 -
CHEMBL2181549 1 -
CHEMBL2387743 1 -
CHEMBL2387744 1 -
CHEMBL2181551 1 -
CHEMBL470199 1 -
CHEMBL2387534 1 -
CHEMBL2387535 1 -
CHEMBL2387539 1 -
CHEMBL2387537 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL465 DRONABINOL Ki = 3.88 nM 8.41
CHEMBL2387530 Ki = 613.0 nM 6.21
CHEMBL2387533 Ki = 3660.0 nM 5.44
CHEMBL2387538 Ki = 7860.0 nM 5.11
CHEMBL2181541 Ki = 10000.0 nM 5.00
CHEMBL2387536 Ki = 10000.0 nM 5.00
CHEMBL2387532 Ki = 10200.0 nM 4.99
CHEMBL2181545 Ki >= 10000.0 nM -
CHEMBL506746 Ki > 10000.0 nM -
CHEMBL470224 Ki > 10000.0 nM -
CHEMBL2181549 Ki > 10000.0 nM -
CHEMBL2387743 Ki > 10000.0 nM -
CHEMBL2387744 Ki > 10000.0 nM -
CHEMBL2181551 Ki > 10000.0 nM -
CHEMBL470199 Ki >= 10000.0 nM -
CHEMBL2387534 Ki >= 10000.0 nM -
CHEMBL2387535 Ki > 10000.0 nM -
CHEMBL2387539 Ki >= 10000.0 nM -
CHEMBL2387537 Ki > 10000.0 nM -