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Assay Detail

CHEMBL828848

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Binding
Inhibitory constant determined against recombinant Fatty-acid amide hydrolase from rat expressed in Escherichia coli
ChEMBL ↗
86
Total Activities
86
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
Boger DL, Miyauchi H, Du W, Hardouin C, Fecik RA, Cheng H, Hwang I, Hedrick MP, Leung D, Acevedo O, Guimarães CR, Jorgensen WL, Cravatt BF.
J Med Chem (2005) 48 : 1849 -1856
PubMed 15771430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 86 7.08 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175580 — — 1 9.85
CHEMBL175854 — — 1 9.70
CHEMBL367966 — — 1 9.55
CHEMBL177757 — — 1 8.66
CHEMBL177922 — — 1 8.64
CHEMBL367009 — — 1 8.48
CHEMBL368284 — — 1 8.34
CHEMBL176122 — — 1 8.34
CHEMBL177577 — — 1 8.33
CHEMBL177858 — — 1 8.28
CHEMBL367307 — — 1 8.25
CHEMBL177729 — — 1 8.24
CHEMBL177708 — — 1 8.12
CHEMBL177216 — — 1 8.11
CHEMBL175950 — — 1 8.05
CHEMBL176173 — — 1 8.00
CHEMBL174397 — — 1 8.00
CHEMBL366959 — — 1 7.96
CHEMBL426232 — — 1 7.96
CHEMBL177356 — — 1 7.92
CHEMBL175833 — — 1 7.92
CHEMBL175695 — — 1 7.89
CHEMBL174917 — — 1 7.85
CHEMBL177788 — — 1 7.82
CHEMBL177686 — — 1 7.80
CHEMBL174052 — — 1 7.80
CHEMBL177226 — — 1 7.80
CHEMBL426230 — — 1 7.75
CHEMBL362061 — — 1 7.75
CHEMBL367859 — — 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175580 — Ki = 0.14 nM 9.85
CHEMBL175854 — Ki = 0.2 nM 9.70
CHEMBL367966 — Ki = 0.28 nM 9.55
CHEMBL177757 — Ki = 2.2 nM 8.66
CHEMBL177922 — Ki = 2.3 nM 8.64
CHEMBL367009 — Ki = 3.3 nM 8.48
CHEMBL368284 — Ki = 4.6 nM 8.34
CHEMBL176122 — Ki = 4.6 nM 8.34
CHEMBL177577 — Ki = 4.7 nM 8.33
CHEMBL177858 — Ki = 5.3 nM 8.28
CHEMBL367307 — Ki = 5.6 nM 8.25
CHEMBL177729 — Ki = 5.8 nM 8.24
CHEMBL177708 — Ki = 7.5 nM 8.12
CHEMBL177216 — Ki = 7.8 nM 8.11
CHEMBL175950 — Ki = 9.0 nM 8.05
CHEMBL176173 — Ki = 10.0 nM 8.00
CHEMBL174397 — Ki = 10.0 nM 8.00
CHEMBL366959 — Ki = 11.0 nM 7.96
CHEMBL426232 — Ki = 11.0 nM 7.96
CHEMBL177356 — Ki = 12.0 nM 7.92
CHEMBL175833 — Ki = 12.0 nM 7.92
CHEMBL175695 — Ki = 13.0 nM 7.89
CHEMBL174917 — Ki = 14.0 nM 7.85
CHEMBL177788 — Ki = 15.0 nM 7.82
CHEMBL177226 — Ki = 16.0 nM 7.80
CHEMBL174052 — Ki = 16.0 nM 7.80
CHEMBL177686 — Ki = 16.0 nM 7.80
CHEMBL426230 — Ki = 18.0 nM 7.75
CHEMBL362061 — Ki = 18.0 nM 7.75
CHEMBL367859 — Ki = 20.0 nM 7.70
CHEMBL175694 — Ki = 21.0 nM 7.68
CHEMBL177245 — Ki = 21.0 nM 7.68
CHEMBL175413 — Ki = 22.0 nM 7.66
CHEMBL175761 — Ki = 22.0 nM 7.66
CHEMBL35925 — Ki = 23.0 nM 7.64
CHEMBL176324 — Ki = 23.0 nM 7.64
CHEMBL91417 — Ki = 25.0 nM 7.60
CHEMBL366671 — Ki = 31.0 nM 7.51
CHEMBL368279 — Ki = 33.0 nM 7.48
CHEMBL176070 — Ki = 41.0 nM 7.39
CHEMBL176166 — Ki = 47.0 nM 7.33
CHEMBL175021 — Ki = 49.0 nM 7.31
CHEMBL174048 — Ki = 54.0 nM 7.27
CHEMBL178071 — Ki = 55.0 nM 7.26
CHEMBL176828 — Ki = 56.0 nM 7.25
CHEMBL174905 — Ki = 59.0 nM 7.23
CHEMBL369547 — Ki = 61.0 nM 7.21
CHEMBL177488 — Ki = 78.0 nM 7.11
CHEMBL422064 — Ki = 80.0 nM 7.10
CHEMBL91416 — Ki = 100.0 nM 7.00