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Assay Detail

CHEMBL953280

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

Binding
Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain membrane in presence of phenylmethanesulfonyl fluoride
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of novel tail-modified anandamide analogs.
Yao F, Li C, Vadivel SK, Bowman AL, Makriyannis A.
Bioorg Med Chem Lett (2008) 18 : 5912 -5915
PubMed 18723350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.96 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473515 1 8.05
CHEMBL462219 1 7.92
CHEMBL460307 1 7.88
CHEMBL120526 METHANANDAMIDE 1 7.75
CHEMBL462593 1 7.52
CHEMBL516986 1 7.16
CHEMBL460306 1 7.12
CHEMBL460485 1 7.05
CHEMBL460486 1 7.02
CHEMBL462572 1 6.77
CHEMBL474733 1 6.77
CHEMBL462608 1 6.62
CHEMBL474531 1 6.55
CHEMBL516663 1 6.49
CHEMBL462607 1 6.46
CHEMBL474532 1 6.46
CHEMBL460487 1 6.27
CHEMBL462573 1 6.25
CHEMBL516628 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473515 Ki = 8.9 nM 8.05
CHEMBL462219 Ki = 12.0 nM 7.92
CHEMBL460307 Ki = 13.3 nM 7.88
CHEMBL120526 METHANANDAMIDE Ki = 17.9 nM 7.75
CHEMBL462593 Ki = 30.4 nM 7.52
CHEMBL516986 Ki = 69.2 nM 7.16
CHEMBL460306 Ki = 76.6 nM 7.12
CHEMBL460485 Ki = 89.4 nM 7.05
CHEMBL460486 Ki = 95.3 nM 7.02
CHEMBL462572 Ki = 170.0 nM 6.77
CHEMBL474733 Ki = 170.0 nM 6.77
CHEMBL462608 Ki = 241.2 nM 6.62
CHEMBL474531 Ki = 284.1 nM 6.55
CHEMBL516663 Ki = 325.0 nM 6.49
CHEMBL462607 Ki = 348.5 nM 6.46
CHEMBL474532 Ki = 344.3 nM 6.46
CHEMBL460487 Ki = 533.3 nM 6.27
CHEMBL462573 Ki = 561.2 nM 6.25
CHEMBL516628 Ki = 678.3 nM 6.17