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Assay Detail

CHEMBL3411462

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

Functional
Cytotoxicity against cIAP/XIAP-dependent human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTS assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-231 (CHEMBL400)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.
Perez HL, Chaudhry C, Emanuel SL, Fanslau C, Fargnoli J, Gan J, Kim KS, Lei M, Naglich JG, Traeger SC, Vuppugalla R, Wei DD, Vite GD, Talbott RL, Borzilleri RM.
J Med Chem (2015) 58 : 1556 -1562
PubMed 25584393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.68 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3410879 1 9.52
CHEMBL3410877 1 9.10
CHEMBL3410878 1 9.05
CHEMBL3410876 1 8.92
CHEMBL3410872 1 8.89
CHEMBL3339214 1 8.82
CHEMBL3410809 1 8.72
CHEMBL3410875 1 8.70
CHEMBL3410871 1 8.57
CHEMBL3410874 1 8.55
CHEMBL3410807 1 8.34
CHEMBL3410808 1 8.21
CHEMBL3410873 1 8.10
CHEMBL3039522 BIRINAPANT 2.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3410879 IC50 = 0.3 nM 9.52
CHEMBL3410877 IC50 = 0.8 nM 9.10
CHEMBL3410878 IC50 = 0.9 nM 9.05
CHEMBL3410876 IC50 = 1.2 nM 8.92
CHEMBL3410872 IC50 = 1.3 nM 8.89
CHEMBL3339214 IC50 = 1.5 nM 8.82
CHEMBL3410809 IC50 = 1.9 nM 8.72
CHEMBL3410875 IC50 = 2.0 nM 8.70
CHEMBL3410871 IC50 = 2.7 nM 8.57
CHEMBL3410874 IC50 = 2.8 nM 8.55
CHEMBL3410807 IC50 = 4.6 nM 8.34
CHEMBL3410808 IC50 = 6.1 nM 8.21
CHEMBL3410873 IC50 = 8.0 nM 8.10
CHEMBL3039522 BIRINAPANT IC50 = 10.0 nM 8.00