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Assay Detail

CHEMBL686015

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

Binding
Inhibition of Fatty-acid amide hydrolase (FAAH) activity in human lymphoma U937 cell using [3H]AEA as substrate in the 0-25 uM conc
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type U-937
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Fatty-acid amide hydrolase 1 (CHEMBL2243)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase.
van der Stelt M, van Kuik JA, Bari M, van Zadelhoff G, Leeflang BR, Veldink GA, Finazzi-Agrò A, Vliegenthart JF, Maccarrone M.
J Med Chem (2002) 45 : 3709 -3720
PubMed 12166944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.80 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440338 1 6.37
CHEMBL333114 1 6.24
CHEMBL122729 1 6.20
CHEMBL331254 1 6.20
CHEMBL122267 1 6.16
CHEMBL126042 1 6.16
CHEMBL331170 1 5.90
CHEMBL121779 1 5.72
CHEMBL262560 1 5.60
CHEMBL121804 1 5.60
CHEMBL121778 1 5.54
CHEMBL124426 1 5.52
CHEMBL332236 1 5.30
CHEMBL122972 2-ARACHIDONOYLGLYCEROL 1 5.30
CHEMBL122195 1 5.22
CHEMBL15848 ANANDAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440338 Ki = 430.0 nM 6.37
CHEMBL333114 Ki = 570.0 nM 6.24
CHEMBL122729 Ki = 630.0 nM 6.20
CHEMBL331254 Ki = 630.0 nM 6.20
CHEMBL122267 Ki = 690.0 nM 6.16
CHEMBL126042 Ki = 690.0 nM 6.16
CHEMBL331170 Ki = 1260.0 nM 5.90
CHEMBL121779 Ki = 1890.0 nM 5.72
CHEMBL262560 Ki = 2500.0 nM 5.60
CHEMBL121804 Ki = 2520.0 nM 5.60
CHEMBL121778 Ki = 2900.0 nM 5.54
CHEMBL124426 Ki = 3000.0 nM 5.52
CHEMBL332236 Ki = 5000.0 nM 5.30
CHEMBL122972 2-ARACHIDONOYLGLYCEROL Ki = 5000.0 nM 5.30
CHEMBL122195 Ki = 6000.0 nM 5.22
CHEMBL15848 ANANDAMIDE Ki > 10000.0 nM -