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Assay Detail

CHEMBL829636

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

Binding
Inhibitor affinity towards enzymes of class serine hydrolase was determined using biotin or fluorescent as radioligand (FP-biotin or FP-Rh)
ChEMBL ↗
42
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
Leung D, Du W, Hardouin C, Cheng H, Hwang I, Cravatt BF, Boger DL.
Bioorg Med Chem Lett (2005) 15 : 1423 -1428
PubMed 15713400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.82 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175854 — — 1 9.70
CHEMBL367966 — — 1 9.55
CHEMBL179359 — — 1 9.54
CHEMBL178398 — — 2 9.54
CHEMBL179760 — — 1 9.41
CHEMBL182199 — — 1 9.28
CHEMBL426967 — — 1 9.25
CHEMBL182206 — — 2 9.11
CHEMBL361529 — — 2 9.08
CHEMBL424976 — — 2 9.07
CHEMBL180625 — — 1 9.00
CHEMBL361170 — — 1 9.00
CHEMBL35925 — — 1 8.64
CHEMBL178563 — — 2 8.52
CHEMBL177577 — — 1 8.33
CHEMBL177708 — — 1 8.12
CHEMBL177216 — — 1 8.11
CHEMBL366959 — — 1 7.96
CHEMBL362705 — — 2 7.80
CHEMBL426230 — — 1 7.75
CHEMBL91417 — — 1 7.60
CHEMBL329187 — — 1 7.10
CHEMBL178791 — — 1 7.05
CHEMBL91416 — — 1 7.00
CHEMBL39412 — — 1 7.00
CHEMBL90258 — — 1 6.89
CHEMBL90308 — — 1 6.85
CHEMBL413727 — — 1 6.77
CHEMBL366907 — — 1 6.66
CHEMBL89946 — — 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175854 — Ki = 0.2 nM 9.70
CHEMBL367966 — Ki = 0.28 nM 9.55
CHEMBL178398 — Ki = 0.29 nM 9.54
CHEMBL179359 — Ki = 0.29 nM 9.54
CHEMBL179760 — Ki = 0.39 nM 9.41
CHEMBL182199 — Ki = 0.52 nM 9.28
CHEMBL426967 — Ki = 0.56 nM 9.25
CHEMBL182206 — Ki = 0.77 nM 9.11
CHEMBL361529 — Ki = 0.83 nM 9.08
CHEMBL424976 — Ki = 0.85 nM 9.07
CHEMBL361529 — Ki = 0.85 nM 9.07
CHEMBL180625 — Ki = 1.0 nM 9.00
CHEMBL361170 — Ki = 1.0 nM 9.00
CHEMBL35925 — Ki = 2.3 nM 8.64
CHEMBL178563 — Ki = 3.0 nM 8.52
CHEMBL178563 — Ki = 3.0 nM 8.52
CHEMBL177577 — Ki = 4.7 nM 8.33
CHEMBL177708 — Ki = 7.5 nM 8.12
CHEMBL177216 — Ki = 7.8 nM 8.11
CHEMBL366959 — Ki = 11.0 nM 7.96
CHEMBL362705 — Ki = 16.0 nM 7.80
CHEMBL362705 — Ki = 16.0 nM 7.80
CHEMBL426230 — Ki = 18.0 nM 7.75
CHEMBL91417 — Ki = 25.0 nM 7.60
CHEMBL329187 — Ki = 80.0 nM 7.10
CHEMBL178791 — Ki = 90.0 nM 7.05
CHEMBL91416 — Ki = 100.0 nM 7.00
CHEMBL39412 — Ki = 100.0 nM 7.00
CHEMBL90258 — Ki = 130.0 nM 6.89
CHEMBL90308 — Ki = 140.0 nM 6.85
CHEMBL413727 — Ki = 170.0 nM 6.77
CHEMBL366907 — Ki = 220.0 nM 6.66
CHEMBL89946 — Ki = 240.0 nM 6.62
CHEMBL178398 — Ki = 290.0 nM 6.54
CHEMBL426410 — Ki = 320.0 nM 6.50
CHEMBL285678 — Ki = 370.0 nM 6.43
CHEMBL424976 — Ki = 560.0 nM 6.25
CHEMBL181668 — Ki = 850.0 nM 6.07
CHEMBL93675 — Ki = 1200.0 nM 5.92
CHEMBL178115 — Ki = 2000.0 nM 5.70
CHEMBL182206 — Ki = 3200.0 nM 5.50
CHEMBL181187 — Ki - nM -