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Assay Detail

CHEMBL2168075

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

Binding
Inhibition of mouse FAAH isolated from brain homogenate using [3H-ethanolamine]AEA as substrate incubated for 20 mins prior to substrate addition measured after 15 mins by beta counting analysis
ChEMBL ↗
42
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fatty-acid amide hydrolase 1 (CHEMBL3455) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases.
Butini S, Brindisi M, Gemma S, Minetti P, Cabri W, Gallo G, Vincenti S, Talamonti E, Borsini F, Caprioli A, Stasi MA, Di Serio S, Ros S, Borrelli G, Maramai S, Fezza F, Campiani G, Maccarrone M.
J Med Chem (2012) 55 : 6898 -6915
PubMed 22779702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.75 9.22
Ki 14 8.33 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165084 — — 2 9.80
CHEMBL2165083 — — 2 9.74
CHEMBL2165094 — — 2 9.31
CHEMBL2165070 — — 2 9.30
CHEMBL184238 URB-597 1.0 2 8.92
CHEMBL2165073 — — 2 8.32
CHEMBL2165080 — — 2 8.15
CHEMBL2165078 — — 2 8.10
CHEMBL2165081 — — 2 7.96
CHEMBL451909 — — 1 7.85
CHEMBL2165079 — — 2 7.75
CHEMBL2165077 — — 2 7.64
CHEMBL2165082 — — 2 7.50
CHEMBL2165095 — — 2 7.22
CHEMBL2165090 — — 2 6.85
CHEMBL2165093 — — 1 -
CHEMBL2165076 — — 1 -
CHEMBL2165075 — — 1 -
CHEMBL2165074 — — 1 -
CHEMBL2165072 — — 1 -
CHEMBL2165071 — — 1 -
CHEMBL2165087 — — 1 -
CHEMBL2165092 — — 1 -
CHEMBL2165091 — — 1 -
CHEMBL2165089 — — 1 -
CHEMBL2165088 — — 1 -
CHEMBL2165085 — — 1 -
CHEMBL2165086 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165084 — Ki = 0.16 nM 9.80
CHEMBL2165083 — Ki = 0.18 nM 9.74
CHEMBL2165094 — Ki = 0.49 nM 9.31
CHEMBL2165070 — Ki = 0.5 nM 9.30
CHEMBL2165084 — IC50 = 0.6 nM 9.22
CHEMBL2165083 — IC50 = 0.67 nM 9.17
CHEMBL184238 URB-597 Ki = 1.2 nM 8.92
CHEMBL2165094 — IC50 = 1.7 nM 8.77
CHEMBL2165070 — IC50 = 1.9 nM 8.72
CHEMBL184238 URB-597 IC50 = 4.6 nM 8.34
CHEMBL2165073 — Ki = 4.8 nM 8.32
CHEMBL2165080 — Ki = 7.0 nM 8.15
CHEMBL2165078 — Ki = 8.0 nM 8.10
CHEMBL2165081 — Ki = 11.0 nM 7.96
CHEMBL451909 — IC50 = 14.0 nM 7.85
CHEMBL2165079 — Ki = 18.0 nM 7.75
CHEMBL2165073 — IC50 = 18.0 nM 7.75
CHEMBL2165077 — Ki = 23.0 nM 7.64
CHEMBL2165080 — IC50 = 28.0 nM 7.55
CHEMBL2165078 — IC50 = 31.0 nM 7.51
CHEMBL2165082 — Ki = 32.0 nM 7.50
CHEMBL2165081 — IC50 = 43.0 nM 7.37
CHEMBL2165095 — Ki = 60.0 nM 7.22
CHEMBL2165079 — IC50 = 69.0 nM 7.16
CHEMBL2165077 — IC50 = 87.0 nM 7.06
CHEMBL2165082 — IC50 = 120.0 nM 6.92
CHEMBL2165090 — Ki = 140.0 nM 6.85
CHEMBL2165095 — IC50 = 240.0 nM 6.62
CHEMBL2165090 — IC50 = 530.0 nM 6.28
CHEMBL2165085 — IC50 > 70.0 nM -
CHEMBL2165086 — IC50 > 200.0 nM -
CHEMBL2165087 — IC50 > 10000.0 nM -
CHEMBL2165088 — IC50 > 50000.0 nM -
CHEMBL2165089 — IC50 > 200.0 nM -
CHEMBL2165076 — IC50 > 200.0 nM -
CHEMBL2165092 — IC50 > 70.0 nM -
CHEMBL2165093 — IC50 > 200.0 nM -
CHEMBL2165071 — IC50 > 200.0 nM -
CHEMBL2165072 — IC50 > 200.0 nM -
CHEMBL2165074 — IC50 > 50000.0 nM -
CHEMBL2165075 — IC50 > 200.0 nM -
CHEMBL2165091 — IC50 > 200.0 nM -