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Assay Detail

CHEMBL4724909

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

Binding
Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in HEK cell membranes incubated for 1.5 hrs by liquid scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
Alghamdi SS,Mustafa SM,Moore Ii BM
Bioorg Med Chem (2021) 33 : 116035 -116035
PubMed 33550084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.48 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764314 1 5.97
CHEMBL4777102 1 5.72
CHEMBL4793741 1 5.43
CHEMBL3907723 1 5.40
CHEMBL460545 1 5.32
CHEMBL4759054 1 5.02
CHEMBL4786835 1 -
CHEMBL4741108 1 -
CHEMBL4776518 1 -
CHEMBL4796513 1 -
CHEMBL4741155 1 -
CHEMBL4755496 1 -
CHEMBL4740459 1 -
CHEMBL4750515 1 -
CHEMBL4752997 1 -
CHEMBL4792566 1 -
CHEMBL4747418 1 -
CHEMBL4785051 1 -
CHEMBL4756251 1 -
CHEMBL4749825 1 -
CHEMBL4752097 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764314 Ki = 1076.0 nM 5.97
CHEMBL4777102 Ki = 1904.0 nM 5.72
CHEMBL4793741 Ki = 3735.0 nM 5.43
CHEMBL3907723 Ki = 4015.0 nM 5.40
CHEMBL460545 Ki = 4778.0 nM 5.32
CHEMBL4759054 Ki = 9526.0 nM 5.02
CHEMBL4786835 Ki > 10000.0 nM -
CHEMBL4741108 Ki > 10000.0 nM -
CHEMBL4776518 Ki > 10000.0 nM -
CHEMBL4796513 Ki > 10000.0 nM -
CHEMBL4741155 Ki > 10000.0 nM -
CHEMBL4755496 Ki > 10000.0 nM -
CHEMBL4740459 Ki > 10000.0 nM -
CHEMBL4750515 Ki > 10000.0 nM -
CHEMBL4752997 Ki > 10000.0 nM -
CHEMBL4792566 Ki > 10000.0 nM -
CHEMBL4747418 Ki > 10000.0 nM -
CHEMBL4785051 Ki > 10000.0 nM -
CHEMBL4756251 Ki > 10000.0 nM -
CHEMBL4749825 Ki > 10000.0 nM -
CHEMBL4752097 Ki > 10000.0 nM -