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Assay Detail

CHEMBL3375436

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

Functional
Inhibition of human XBP1 splicing in human HT1080-CMV-XBP1-Luciferase cells assessed as luciferase signal by Promega Bright-Glo luciferase assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-1080
Confidence 1 — Organism
Curated By Autocuration

Target

HT-1080 (CHEMBL614580)
Type CELL-LINE
Organism Homo sapiens

Publication

Unfolded Protein Response in Cancer: IRE1α Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability.
Harrington PE, Biswas K, Malwitz D, Tasker AS, Mohr C, Andrews KL, Dellamaggiore K, Kendall R, Beckmann H, Jaeckel P, Materna-Reichelt S, Allen JR, Lipford JR.
ACS Med Chem Lett (2015) 6 : 68 -72
PubMed 25589933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.76 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356002 1 7.89
CHEMBL3355998 1 7.51
CHEMBL3355999 1 7.48
CHEMBL3356001 1 7.48
CHEMBL3356007 1 7.38
CHEMBL3356003 1 7.29
CHEMBL3356006 1 7.21
CHEMBL3356009 1 7.00
CHEMBL3356008 1 6.92
CHEMBL3355993 1 6.70
CHEMBL3355992 1 6.57
CHEMBL3355996 1 6.51
CHEMBL3356000 1 6.47
CHEMBL3356005 1 6.36
CHEMBL3356010 1 6.24
CHEMBL3355997 1 6.24
CHEMBL3356004 1 6.23
CHEMBL3355995 1 6.06
CHEMBL3355994 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356002 IC50 = 13.0 nM 7.89
CHEMBL3355998 IC50 = 31.0 nM 7.51
CHEMBL3355999 IC50 = 33.0 nM 7.48
CHEMBL3356001 IC50 = 33.0 nM 7.48
CHEMBL3356007 IC50 = 42.0 nM 7.38
CHEMBL3356003 IC50 = 51.0 nM 7.29
CHEMBL3356006 IC50 = 62.0 nM 7.21
CHEMBL3356009 IC50 = 99.0 nM 7.00
CHEMBL3356008 IC50 = 120.0 nM 6.92
CHEMBL3355993 IC50 = 200.0 nM 6.70
CHEMBL3355992 IC50 = 270.0 nM 6.57
CHEMBL3355996 IC50 = 310.0 nM 6.51
CHEMBL3356000 IC50 = 340.0 nM 6.47
CHEMBL3356005 IC50 = 440.0 nM 6.36
CHEMBL3356010 IC50 = 580.0 nM 6.24
CHEMBL3355997 IC50 = 570.0 nM 6.24
CHEMBL3356004 IC50 = 590.0 nM 6.23
CHEMBL3355995 IC50 = 870.0 nM 6.06
CHEMBL3355994 IC50 = 15000.0 nM 4.82