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Assay Detail

CHEMBL1763765

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

Binding
Inhibition of rat FAAH assessed as hydrolysis of anandamido-amino-methyl-cumarin
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F.
Bioorg Med Chem Lett (2011) 21 : 2492 -2496
PubMed 21392988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 7.03 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184238 URB-597 1.0 1 8.52
CHEMBL472535 1 8.52
CHEMBL1761301 1 8.40
CHEMBL1761302 1 8.10
CHEMBL460273 1 8.00
CHEMBL1761284 1 8.00
CHEMBL1761455 1 7.75
CHEMBL366959 1 7.60
CHEMBL1761303 1 7.58
CHEMBL1761299 1 7.52
CHEMBL1761279 1 7.44
CHEMBL1761457 1 7.41
CHEMBL1761304 1 7.37
CHEMBL1761456 1 7.28
CHEMBL1761282 1 7.22
CHEMBL1761307 1 7.12
CHEMBL1761308 1 7.12
CHEMBL1761306 1 7.08
CHEMBL1761295 1 6.92
CHEMBL1761305 1 6.92
CHEMBL1761296 1 6.80
CHEMBL1761300 1 6.72
CHEMBL1761291 1 6.70
CHEMBL1761292 1 6.66
CHEMBL1761297 1 6.55
CHEMBL1761289 1 6.52
CHEMBL1761298 1 6.47
CHEMBL1761290 1 6.24
CHEMBL1761281 1 6.11
CHEMBL1761294 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184238 URB-597 IC50 = 3.0 nM 8.52
CHEMBL472535 IC50 = 3.0 nM 8.52
CHEMBL1761301 IC50 = 4.0 nM 8.40
CHEMBL1761302 IC50 = 8.0 nM 8.10
CHEMBL460273 IC50 = 10.0 nM 8.00
CHEMBL1761284 IC50 = 10.0 nM 8.00
CHEMBL1761455 IC50 = 18.0 nM 7.75
CHEMBL366959 IC50 = 25.0 nM 7.60
CHEMBL1761303 IC50 = 26.0 nM 7.58
CHEMBL1761299 IC50 = 30.0 nM 7.52
CHEMBL1761279 IC50 = 36.0 nM 7.44
CHEMBL1761457 IC50 = 39.0 nM 7.41
CHEMBL1761304 IC50 = 43.0 nM 7.37
CHEMBL1761456 IC50 = 53.0 nM 7.28
CHEMBL1761282 IC50 = 60.0 nM 7.22
CHEMBL1761307 IC50 = 75.0 nM 7.12
CHEMBL1761308 IC50 = 75.0 nM 7.12
CHEMBL1761306 IC50 = 83.0 nM 7.08
CHEMBL1761295 IC50 = 120.0 nM 6.92
CHEMBL1761305 IC50 = 120.0 nM 6.92
CHEMBL1761296 IC50 = 160.0 nM 6.80
CHEMBL1761300 IC50 = 190.0 nM 6.72
CHEMBL1761291 IC50 = 200.0 nM 6.70
CHEMBL1761292 IC50 = 220.0 nM 6.66
CHEMBL1761297 IC50 = 280.0 nM 6.55
CHEMBL1761289 IC50 = 300.0 nM 6.52
CHEMBL1761298 IC50 = 340.0 nM 6.47
CHEMBL1761290 IC50 = 570.0 nM 6.24
CHEMBL1761281 IC50 = 780.0 nM 6.11
CHEMBL1761294 IC50 = 1200.0 nM 5.92
CHEMBL1761293 IC50 = 3000.0 nM 5.52
CHEMBL1761288 IC50 = 10000.0 nM 5.00
CHEMBL1761458 IC50 = 10000.0 nM 5.00
CHEMBL1761277 IC50 > 10000.0 nM -
CHEMBL1761278 IC50 > 10000.0 nM -
CHEMBL1761280 IC50 > 10000.0 nM -
CHEMBL1761283 IC50 > 10000.0 nM -
CHEMBL1761285 IC50 > 10000.0 nM -
CHEMBL1761286 IC50 > 10000.0 nM -
CHEMBL1761287 IC50 > 10000.0 nM -