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Assay Detail

CHEMBL5730291

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Binding
Fluorescence Polarization Assay: Assays were performed in black, flat-bottom, 384-well plates. The final assay volume was 50 μL prepared from additions of N-His-Tb-BIR3(241-356, XIAP), fluoresceinated modified SMAC peptide, and test compounds in assay buffer consisting of 20 mM Sodium Phosphate, 1 mM EDTA, 50 mM NaCl, and 0.05% PLURONIC® F68. The reaction was incubated at room temperature for 60 minutes and fluorescence polarization of the reaction was detected on the LJL Plate Reader Inhibition data were calculated from mP values generated by the no protein control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assay was 130 nM N-His-Tb-BIR3(241-356, XIAP), 1.4 nM fluoresceinated modified SMAC peptide, and 1% DMSO.
ChEMBL ↗
57
Total Activities
17
Compounds Tested
3
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

IAP antagonists
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 9.90 10.22
kon 19 - -
k_off 19 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3918792 — — 3 10.22
CHEMBL3929256 — — 6 10.22
CHEMBL3940255 — — 3 10.22
CHEMBL3913296 — — 3 10.22
CHEMBL3930765 — — 3 10.15
CHEMBL3950036 — — 3 10.10
CHEMBL3903824 — — 3 10.10
CHEMBL3976012 — — 3 9.89
CHEMBL3941276 — — 3 9.85
CHEMBL3927714 — — 3 9.85
CHEMBL3950322 — — 3 9.85
CHEMBL3940832 — — 6 9.82
CHEMBL3896723 — — 3 9.80
CHEMBL3917007 — — 3 9.74
CHEMBL3946177 — — 3 9.68
CHEMBL3918274 — — 3 9.66
CHEMBL3954865 — — 3 9.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3940255 — IC50 = 0.06 nM 10.22
CHEMBL3913296 — IC50 = 0.06 nM 10.22
CHEMBL3929256 — IC50 = 0.06 nM 10.22
CHEMBL3918792 — IC50 = 0.06 nM 10.22
CHEMBL3930765 — IC50 = 0.07 nM 10.15
CHEMBL3903824 — IC50 = 0.08 nM 10.10
CHEMBL3950036 — IC50 = 0.08 nM 10.10
CHEMBL3976012 — IC50 = 0.13 nM 9.89
CHEMBL3950322 — IC50 = 0.14 nM 9.85
CHEMBL3927714 — IC50 = 0.14 nM 9.85
CHEMBL3941276 — IC50 = 0.14 nM 9.85
CHEMBL3940832 — IC50 = 0.15 nM 9.82
CHEMBL3896723 — IC50 = 0.16 nM 9.80
CHEMBL3917007 — IC50 = 0.18 nM 9.74
CHEMBL3946177 — IC50 = 0.21 nM 9.68
CHEMBL3918274 — IC50 = 0.22 nM 9.66
CHEMBL3940832 — IC50 = 0.23 nM 9.64
CHEMBL3929256 — IC50 = 0.25 nM 9.60
CHEMBL3954865 — IC50 = 0.27 nM 9.57
CHEMBL3950322 — k_off = - s-1 -
CHEMBL3950322 — kon = - — -
CHEMBL3927714 — k_off = - s-1 -
CHEMBL3940832 — kon = - — -
CHEMBL3896723 — k_off = - s-1 -
CHEMBL3896723 — kon = - — -
CHEMBL3918792 — k_off = - s-1 -
CHEMBL3918792 — kon = - — -
CHEMBL3950036 — k_off = - s-1 -
CHEMBL3950036 — kon = - — -
CHEMBL3913296 — k_off = - s-1 -
CHEMBL3913296 — kon = - — -
CHEMBL3941276 — k_off = - s-1 -
CHEMBL3941276 — kon = - — -
CHEMBL3927714 — kon = - — -
CHEMBL3917007 — k_off = - s-1 -
CHEMBL3917007 — kon = - — -
CHEMBL3946177 — k_off = - s-1 -
CHEMBL3946177 — kon = - — -
CHEMBL3918274 — k_off = - s-1 -
CHEMBL3918274 — kon = - — -
CHEMBL3954865 — k_off = - s-1 -
CHEMBL3954865 — kon = - — -
CHEMBL3930765 — k_off = - s-1 -
CHEMBL3930765 — kon = - — -
CHEMBL3940832 — k_off = - s-1 -
CHEMBL3929256 — kon = - — -
CHEMBL3903824 — kon = - — -
CHEMBL3940832 — kon = - — -
CHEMBL3903824 — k_off = - s-1 -
CHEMBL3940832 — k_off = - s-1 -