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Assay Detail

CHEMBL978248

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

Binding
Inhibition of rat FAAH preincubated for 20 mins
26
Total Activities
26
Compounds Tested
2
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

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG.
Bioorg Med Chem Lett (2008) 18 : 4838 -4843
PubMed 18693015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.79 8.21
Ki 1 8.33 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177577 1 8.33
CHEMBL472535 1 8.21
CHEMBL461935 1 7.74
CHEMBL460273 1 7.47
CHEMBL461380 1 7.33
CHEMBL184238 URB-597 1.0 1 7.32
CHEMBL461942 1 7.08
CHEMBL518812 1 7.04
CHEMBL472529 1 6.93
CHEMBL472188 1 6.91
CHEMBL472187 1 6.83
CHEMBL518653 1 6.83
CHEMBL472534 1 6.82
CHEMBL461753 1 6.79
CHEMBL472530 1 6.61
CHEMBL516650 1 6.55
CHEMBL472189 1 6.52
CHEMBL461752 1 6.46
CHEMBL512882 1 6.46
CHEMBL461569 1 5.90
CHEMBL518657 1 5.78
CHEMBL470107 1 5.08
CHEMBL470108 1 -
CHEMBL471155 1 -
CHEMBL471320 1 -
CHEMBL471321 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177577 Ki = 4.7 nM 8.33
CHEMBL472535 IC50 = 6.2 nM 8.21
CHEMBL461935 IC50 = 18.3 nM 7.74
CHEMBL460273 IC50 = 34.0 nM 7.47
CHEMBL461380 IC50 = 47.0 nM 7.33
CHEMBL184238 URB-597 IC50 = 48.0 nM 7.32
CHEMBL461942 IC50 = 84.0 nM 7.08
CHEMBL518812 IC50 = 91.0 nM 7.04
CHEMBL472529 IC50 = 117.0 nM 6.93
CHEMBL472188 IC50 = 122.0 nM 6.91
CHEMBL472187 IC50 = 147.0 nM 6.83
CHEMBL518653 IC50 = 148.0 nM 6.83
CHEMBL472534 IC50 = 152.0 nM 6.82
CHEMBL461753 IC50 = 163.0 nM 6.79
CHEMBL472530 IC50 = 248.0 nM 6.61
CHEMBL516650 IC50 = 280.0 nM 6.55
CHEMBL472189 IC50 = 300.0 nM 6.52
CHEMBL461752 IC50 = 350.0 nM 6.46
CHEMBL512882 IC50 = 350.0 nM 6.46
CHEMBL461569 IC50 = 1270.0 nM 5.90
CHEMBL518657 IC50 = 1666.0 nM 5.78
CHEMBL470107 IC50 = 8330.0 nM 5.08
CHEMBL470108 IC50 > 10000.0 nM -
CHEMBL471155 IC50 > 10000.0 nM -
CHEMBL471320 IC50 > 10000.0 nM -
CHEMBL471321 IC50 > 10000.0 nM -