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Assay Detail

CHEMBL3874926

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

Binding
Inhibition of FAAH in rat brain microsomes using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate after 60 mins by fluorescence-based reversed phase HPLC analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
Zahov S, Garzinsky D, Hanekamp W, Lehr M.
Bioorg Med Chem (2017) 25 : 825 -837
PubMed 27989417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.15 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175854 1 8.54
CHEMBL3897053 1 8.05
CHEMBL3917532 1 8.00
CHEMBL3906001 1 7.96
CHEMBL3973827 1 7.96
CHEMBL3924002 1 7.92
CHEMBL3954141 1 7.92
CHEMBL3935429 1 7.92
CHEMBL3957353 1 7.89
CHEMBL3932943 1 7.89
CHEMBL3962880 1 7.85
CHEMBL590142 1 7.82
CHEMBL3933992 1 7.72
CHEMBL3944384 1 7.68
CHEMBL3936528 1 7.41
CHEMBL3918133 1 7.37
CHEMBL3976882 1 7.31
CHEMBL3908582 1 7.28
CHEMBL184238 URB-597 1.0 1 7.22
CHEMBL3968351 1 7.03
CHEMBL3921983 1 7.00
CHEMBL598974 1 6.39
CHEMBL3986042 1 6.39
CHEMBL590143 1 6.32
CHEMBL3906192 1 6.21
CHEMBL3960423 1 6.20
CHEMBL592145 1 6.08
CHEMBL3938779 1 5.80
CHEMBL3951706 1 5.75
CHEMBL603330 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175854 IC50 = 2.9 nM 8.54
CHEMBL3897053 IC50 = 9.0 nM 8.05
CHEMBL3917532 IC50 = 10.0 nM 8.00
CHEMBL3906001 IC50 = 11.0 nM 7.96
CHEMBL3973827 IC50 = 11.0 nM 7.96
CHEMBL3924002 IC50 = 12.0 nM 7.92
CHEMBL3954141 IC50 = 12.0 nM 7.92
CHEMBL3935429 IC50 = 12.0 nM 7.92
CHEMBL3957353 IC50 = 13.0 nM 7.89
CHEMBL3932943 IC50 = 13.0 nM 7.89
CHEMBL3962880 IC50 = 14.0 nM 7.85
CHEMBL590142 IC50 = 15.0 nM 7.82
CHEMBL3933992 IC50 = 19.0 nM 7.72
CHEMBL3944384 IC50 = 21.0 nM 7.68
CHEMBL3936528 IC50 = 39.0 nM 7.41
CHEMBL3918133 IC50 = 43.0 nM 7.37
CHEMBL3976882 IC50 = 49.0 nM 7.31
CHEMBL3908582 IC50 = 53.0 nM 7.28
CHEMBL184238 URB-597 IC50 = 60.0 nM 7.22
CHEMBL3968351 IC50 = 93.0 nM 7.03
CHEMBL3921983 IC50 = 100.0 nM 7.00
CHEMBL598974 IC50 = 410.0 nM 6.39
CHEMBL3986042 IC50 = 410.0 nM 6.39
CHEMBL590143 IC50 = 480.0 nM 6.32
CHEMBL3906192 IC50 = 620.0 nM 6.21
CHEMBL3960423 IC50 = 630.0 nM 6.20
CHEMBL592145 IC50 = 840.0 nM 6.08
CHEMBL3938779 IC50 = 1600.0 nM 5.80
CHEMBL3951706 IC50 = 1800.0 nM 5.75
CHEMBL603330 IC50 = 2300.0 nM 5.64
CHEMBL3925106 IC50 = 6300.0 nM 5.20
CHEMBL3936085 IC50 > 10000.0 nM -
CHEMBL3914980 IC50 > 10000.0 nM -