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Assay Detail

CHEMBL873899

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

Functional
Ability to inhibit [3H]anandamide uptake in human lymphoma U937 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Expert

Target

U-937 (CHEMBL612794)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
López-Rodríguez ML, Viso A, Ortega-Gutiérrez S, Lastres-Becker I, González S, Fernández-Ruiz J, Ramos JA.
J Med Chem (2001) 44 : 4505 -4508
PubMed 11741470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.22 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434778 1 6.10
CHEMBL284300 1 5.52
CHEMBL39878 1 5.40
CHEMBL39460 1 5.30
CHEMBL417158 1 5.30
CHEMBL431128 1 5.24
CHEMBL287130 1 5.10
CHEMBL290716 1 4.85
CHEMBL287364 1 4.75
CHEMBL38293 1 4.62
CHEMBL287788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434778 IC50 = 800.0 nM 6.10
CHEMBL284300 IC50 = 3000.0 nM 5.52
CHEMBL39878 IC50 = 4000.0 nM 5.40
CHEMBL39460 IC50 = 5000.0 nM 5.30
CHEMBL417158 IC50 = 5000.0 nM 5.30
CHEMBL431128 IC50 = 5700.0 nM 5.24
CHEMBL287130 IC50 = 8000.0 nM 5.10
CHEMBL290716 IC50 = 14000.0 nM 4.85
CHEMBL287364 IC50 = 18000.0 nM 4.75
CHEMBL38293 IC50 = 24000.0 nM 4.62
CHEMBL287788 IC50 = - nM -