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Assay Detail

CHEMBL954831

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

Binding
Inhibition of FAAH in rat brain membrane assessed as [3H]anandamide hydrolysis
ChEMBL ↗
52
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
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 quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.
Mor M, Lodola A, Rivara S, Vacondio F, Duranti A, Tontini A, Sanchini S, Piersanti G, Clapper JR, King AR, Tarzia G, Piomelli D.
J Med Chem (2008) 51 : 3487 -3498
PubMed 18507372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.99 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483697 — — 1 9.20
CHEMBL184238 URB-597 1.0 1 8.34
CHEMBL520890 — — 1 8.28
CHEMBL521228 — — 2 8.28
CHEMBL486701 — — 2 8.27
CHEMBL487534 — — 2 8.11
CHEMBL486492 — — 2 8.03
CHEMBL486493 — — 2 7.89
CHEMBL448753 — — 2 7.47
CHEMBL486700 — — 2 7.40
CHEMBL487317 — — 2 7.28
CHEMBL451441 — — 2 7.27
CHEMBL488348 — — 2 7.24
CHEMBL487121 — — 2 7.23
CHEMBL431202 — — 2 7.20
CHEMBL485685 — — 2 7.18
CHEMBL446837 — — 2 6.95
CHEMBL485689 — — 2 6.86
CHEMBL449538 — — 2 6.76
CHEMBL485886 — — 2 6.67
CHEMBL485686 — — 1 6.61
CHEMBL520360 — — 2 6.32
CHEMBL486494 — — 2 6.28
CHEMBL451174 — — 2 6.16
CHEMBL505895 — — 1 5.59
CHEMBL451443 — — 1 5.51
CHEMBL487535 — — 1 5.40
CHEMBL485883 — — 2 5.39
CHEMBL486290 — — 2 4.86
CHEMBL488339 — — 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483697 — IC50 = 0.63 nM 9.20
CHEMBL184238 URB-597 IC50 = 4.6 nM 8.34
CHEMBL520890 — IC50 = 5.2 nM 8.28
CHEMBL521228 — IC50 = 5.3 nM 8.28
CHEMBL486701 — IC50 = 5.37 nM 8.27
CHEMBL521228 — IC50 = 5.37 nM 8.27
CHEMBL486701 — IC50 = 5.4 nM 8.27
CHEMBL487534 — IC50 = 7.8 nM 8.11
CHEMBL487534 — IC50 = 7.762 nM 8.11
CHEMBL486492 — IC50 = 9.333 nM 8.03
CHEMBL486492 — IC50 = 9.4 nM 8.03
CHEMBL486493 — IC50 = 12.88 nM 7.89
CHEMBL486493 — IC50 = 13.0 nM 7.89
CHEMBL448753 — IC50 = 34.0 nM 7.47
CHEMBL448753 — IC50 = 33.88 nM 7.47
CHEMBL486700 — IC50 = 39.9 nM 7.40
CHEMBL486700 — IC50 = 39.81 nM 7.40
CHEMBL487317 — IC50 = 52.48 nM 7.28
CHEMBL487317 — IC50 = 53.0 nM 7.28
CHEMBL451441 — IC50 = 53.7 nM 7.27
CHEMBL451441 — IC50 = 54.0 nM 7.27
CHEMBL488348 — IC50 = 57.54 nM 7.24
CHEMBL488348 — IC50 = 57.0 nM 7.24
CHEMBL487121 — IC50 = 59.0 nM 7.23
CHEMBL487121 — IC50 = 58.88 nM 7.23
CHEMBL431202 — IC50 = 63.0 nM 7.20
CHEMBL431202 — IC50 = 63.1 nM 7.20
CHEMBL485685 — IC50 = 66.07 nM 7.18
CHEMBL485685 — IC50 = 66.0 nM 7.18
CHEMBL446837 — IC50 = 113.0 nM 6.95
CHEMBL446837 — IC50 = 112.2 nM 6.95
CHEMBL485689 — IC50 = 139.0 nM 6.86
CHEMBL485689 — IC50 = 138.04 nM 6.86
CHEMBL449538 — IC50 = 175.0 nM 6.76
CHEMBL449538 — IC50 = 173.78 nM 6.76
CHEMBL485886 — IC50 = 215.0 nM 6.67
CHEMBL485886 — IC50 = 213.8 nM 6.67
CHEMBL485686 — IC50 = 244.0 nM 6.61
CHEMBL520360 — IC50 = 481.0 nM 6.32
CHEMBL520360 — IC50 = 478.63 nM 6.32
CHEMBL486494 — IC50 = 524.81 nM 6.28
CHEMBL486494 — IC50 = 521.0 nM 6.28
CHEMBL451174 — IC50 = 691.83 nM 6.16
CHEMBL451174 — IC50 = 696.0 nM 6.16
CHEMBL505895 — IC50 = 2551.0 nM 5.59
CHEMBL451443 — IC50 = 3091.0 nM 5.51
CHEMBL487535 — IC50 = 3942.0 nM 5.40
CHEMBL485883 — IC50 = 4089.0 nM 5.39
CHEMBL485883 — IC50 = 4073.8 nM 5.39
CHEMBL486290 — IC50 = 13803.84 nM 4.86