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Assay Detail

CHEMBL1065613

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

Binding
Inhibition of FAAH-mediated [3H]AEA hydrolysis in rat brain homogenate by liquid scintillation spectroscopy
40
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fatty-acid amide hydrolase 1 (CHEMBL3229)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors.
Onnis V, Congiu C, Björklund E, Hempel F, Söderström E, Fowler CJ.
J Med Chem (2010) 53 : 2286 -2298
PubMed 20143779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.36 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL599617 2 7.00
CHEMBL597562 2 6.75
CHEMBL591932 2 6.14
CHEMBL605981 2 6.06
CHEMBL596757 2 5.89
CHEMBL606391 2 5.82
CHEMBL599823 2 5.59
CHEMBL597360 2 5.57
CHEMBL599618 2 5.53
CHEMBL590986 2 5.37
CHEMBL597561 2 5.34
CHEMBL599195 2 5.06
CHEMBL603879 2 4.66
CHEMBL605348 2 4.51
CHEMBL597149 2 4.42
CHEMBL598165 2 4.33
CHEMBL599196 2 4.24
CHEMBL604295 2 4.19
CHEMBL605568 1 -
CHEMBL112 ACETAMINOPHEN 4.0 1 -
CHEMBL521 IBUPROFEN 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL599617 IC50 = 100.0 nM 7.00
CHEMBL599617 IC50 = 100.0 nM 7.00
CHEMBL597562 IC50 = 180.0 nM 6.75
CHEMBL597562 IC50 = 181.97 nM 6.74
CHEMBL591932 IC50 = 730.0 nM 6.14
CHEMBL591932 IC50 = 724.44 nM 6.14
CHEMBL605981 IC50 = 870.0 nM 6.06
CHEMBL605981 IC50 = 870.96 nM 6.06
CHEMBL596757 IC50 = 1300.0 nM 5.89
CHEMBL596757 IC50 = 1318.26 nM 5.88
CHEMBL606391 IC50 = 1513.56 nM 5.82
CHEMBL606391 IC50 = 1500.0 nM 5.82
CHEMBL599823 IC50 = 2570.4 nM 5.59
CHEMBL599823 IC50 = 2600.0 nM 5.58
CHEMBL597360 IC50 = 2691.53 nM 5.57
CHEMBL597360 IC50 = 2700.0 nM 5.57
CHEMBL599618 IC50 = 2951.21 nM 5.53
CHEMBL599618 IC50 = 3000.0 nM 5.52
CHEMBL590986 IC50 = 4265.8 nM 5.37
CHEMBL590986 IC50 = 4300.0 nM 5.37
CHEMBL597561 IC50 = 4600.0 nM 5.34
CHEMBL597561 IC50 = 4570.88 nM 5.34
CHEMBL599195 IC50 = 8700.0 nM 5.06
CHEMBL599195 IC50 = 8709.64 nM 5.06
CHEMBL603879 IC50 = 21877.62 nM 4.66
CHEMBL603879 IC50 = 22000.0 nM 4.66
CHEMBL605348 IC50 = 30902.95 nM 4.51
CHEMBL605348 IC50 = 31000.0 nM 4.51
CHEMBL597149 IC50 = 38018.94 nM 4.42
CHEMBL597149 IC50 = 38000.0 nM 4.42
CHEMBL598165 IC50 = 47000.0 nM 4.33
CHEMBL598165 IC50 = 46773.51 nM 4.33
CHEMBL599196 IC50 = 58000.0 nM 4.24
CHEMBL599196 IC50 = 57543.99 nM 4.24
CHEMBL604295 IC50 = 64565.42 nM 4.19
CHEMBL604295 IC50 = 64000.0 nM 4.19
CHEMBL521 IBUPROFEN IC50 = 260000.0 nM -
CHEMBL112 ACETAMINOPHEN IC50 > 300000.0 nM -
CHEMBL605568 IC50 > 300000.0 nM -
CHEMBL521 IBUPROFEN IC50 = 263026.8 nM -