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Assay Detail

CHEMBL2072019

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

Binding
Inhibition of human KIAA1363 expressed in 293T/17 cells using 2-thioacetyl MAGE as substrate preincubated for 4 hrs measured after 1 hr
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neutral cholesterol ester hydrolase 1 (CHEMBL5048)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).
Shreder KR, Lin EC, Wu J, Cajica J, Amantea CM, Hu Y, Okerberg E, Brown HE, Pham LM, Chung de M, Fraser AS, McGee E, Rosenblum JS, Kozarich JW.
Bioorg Med Chem Lett (2012) 22 : 5748 -5751
PubMed 22877630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.12 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2069333 1 7.00
CHEMBL2071656 1 6.48
CHEMBL2071659 1 6.15
CHEMBL2069332 1 5.96
CHEMBL2071658 1 5.82
CHEMBL2071626 1 5.77
CHEMBL2071657 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2069333 IC50 = 100.0 nM 7.00
CHEMBL2071656 IC50 = 330.0 nM 6.48
CHEMBL2071659 IC50 = 710.0 nM 6.15
CHEMBL2069332 IC50 = 1100.0 nM 5.96
CHEMBL2071658 IC50 = 1500.0 nM 5.82
CHEMBL2071626 IC50 = 1700.0 nM 5.77
CHEMBL2071657 IC50 = 2200.0 nM 5.66