Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL657981

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

Binding
In vitro inhibition of carboxylesterase in human liver microsomes.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cocaine esterase (CHEMBL3180)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors.
Wheelock CE, Colvin ME, Uemura I, Olmstead MM, Sanborn JR, Nakagawa Y, Jones AD, Hammock BD.
J Med Chem (2002) 45 : 5576 -5593
PubMed 12459025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.56 9.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155514 1 9.75
CHEMBL155513 1 8.47
CHEMBL153080 1 8.26
CHEMBL440542 1 8.16
CHEMBL153015 1 7.49
CHEMBL155621 1 7.33
CHEMBL421992 1 7.32
CHEMBL153177 1 7.00
CHEMBL155396 1 6.51
CHEMBL152225 1 5.69
CHEMBL152843 1 5.36
CHEMBL152698 1 5.30
CHEMBL152376 1 4.93
CHEMBL153107 1 4.55
CHEMBL150821 1 4.54
CHEMBL153556 1 4.26
CHEMBL153601 1 -
CHEMBL356917 1 -
CHEMBL150648 1 -
CHEMBL152577 1 -
CHEMBL47127 2-DECANONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155514 IC50 = 0.1778 nM 9.75
CHEMBL155513 IC50 = 3.388 nM 8.47
CHEMBL153080 IC50 = 5.495 nM 8.26
CHEMBL440542 IC50 = 6.918 nM 8.16
CHEMBL153015 IC50 = 32.36 nM 7.49
CHEMBL155621 IC50 = 46.77 nM 7.33
CHEMBL421992 IC50 = 47.86 nM 7.32
CHEMBL153177 IC50 = 100.0 nM 7.00
CHEMBL155396 IC50 = 309.03 nM 6.51
CHEMBL152225 IC50 = 2041.74 nM 5.69
CHEMBL152843 IC50 = 4365.16 nM 5.36
CHEMBL152698 IC50 = 5011.87 nM 5.30
CHEMBL152376 IC50 = 11748.98 nM 4.93
CHEMBL153107 IC50 = 28183.83 nM 4.55
CHEMBL150821 IC50 = 28840.32 nM 4.54
CHEMBL153556 IC50 = 54954.09 nM 4.26
CHEMBL153601 IC50 = 141253.75 nM -
CHEMBL356917 IC50 = 158489.32 nM -
CHEMBL150648 IC50 = 933254.3 nM -
CHEMBL152577 IC50 = 104712.85 nM -
CHEMBL47127 2-DECANONE IC50 = 8511380.38 nM -