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Assay Detail

CHEMBL4305437

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

Binding
Displacement of biotinylated AVPF from N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 8 hrs by DELFIA
13
Total Activities
13
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

E3 ubiquitin-protein ligase XIAP (CHEMBL4198)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
Gambini L, Baggio C, Udompholkul P, Jossart J, Salem AF, Perry JJP, Pellecchia M.
J Med Chem (2019) 62 : 5616 -5627
PubMed 31095386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.48 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443905 1 8.46
CHEMBL4475136 1 8.10
CHEMBL4277819 1 7.89
CHEMBL2063869 GDC-0152 1.0 1 7.68
CHEMBL4545874 1 7.62
CHEMBL4437401 1 7.55
CHEMBL4283320 1 7.41
CHEMBL2431768 LCL-161 2.0 1 7.28
CHEMBL4555169 1 7.19
CHEMBL4462680 1 7.05
CHEMBL4464994 1 7.00
CHEMBL4437384 1 7.00
CHEMBL4472035 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443905 IC50 = 3.5 nM 8.46
CHEMBL4475136 IC50 = 8.0 nM 8.10
CHEMBL4277819 IC50 = 13.0 nM 7.89
CHEMBL2063869 GDC-0152 IC50 = 21.0 nM 7.68
CHEMBL4545874 IC50 = 24.0 nM 7.62
CHEMBL4437401 IC50 = 28.0 nM 7.55
CHEMBL4283320 IC50 = 39.0 nM 7.41
CHEMBL2431768 LCL-161 IC50 = 53.0 nM 7.28
CHEMBL4555169 IC50 = 65.0 nM 7.19
CHEMBL4462680 IC50 = 90.0 nM 7.05
CHEMBL4464994 IC50 = 100.0 nM 7.00
CHEMBL4437384 IC50 = 100.0 nM 7.00
CHEMBL4472035 IC50 = 105.0 nM 6.98