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Assay Detail

CHEMBL5526697

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

Binding
Inhibition of XPO1 in human Jurkat cells assessed as suppression of IL-2 expression incubated for 6 hrs by Bright-Glo Luciferase based microplate reader analysis
46
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Exportin-1 (CHEMBL5661)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules.
Chen YF, Shen Y, Yan DF, Ghazala M, Scemama de Gialluly MA, Srinivasan R, Farrar AN, Friedrich RM, Adams DJ.
J Med Chem (2024) 67 : 12033 -12054
PubMed 39005064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 46 7.01 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129857 AS-602868 1.0 1 8.70
CHEMBL5559223 1 8.40
CHEMBL5555068 2 8.40
CHEMBL5556912 1 8.40
CHEMBL3898452 1 8.30
CHEMBL5568605 1 8.15
CHEMBL5542885 1 7.96
CHEMBL3545185 SELINEXOR 4.0 1 7.92
CHEMBL5566091 1 7.89
CHEMBL5560534 1 7.72
CHEMBL5564554 1 7.68
CHEMBL5563530 1 7.64
CHEMBL3545187 VERDINEXOR 2.0 1 7.62
CHEMBL5562376 1 7.62
CHEMBL5542505 1 7.60
CHEMBL5542934 1 7.58
CHEMBL5561373 1 7.40
CHEMBL130837 1 7.32
CHEMBL5556828 1 7.26
CHEMBL5563179 1 7.24
CHEMBL5562296 1 7.19
CHEMBL130007 1 7.09
CHEMBL5566432 1 7.08
CHEMBL5564519 1 7.04
CHEMBL336546 1 6.97
CHEMBL5566341 1 6.86
CHEMBL5555764 1 6.86
CHEMBL5561263 1 6.84
CHEMBL5560350 1 6.69
CHEMBL5565311 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129857 AS-602868 EC50 = 2.0 nM 8.70
CHEMBL5559223 EC50 = 4.0 nM 8.40
CHEMBL5555068 EC50 = 4.0 nM 8.40
CHEMBL5556912 EC50 = 4.0 nM 8.40
CHEMBL3898452 EC50 = 5.0 nM 8.30
CHEMBL5555068 EC50 = 6.0 nM 8.22
CHEMBL5568605 EC50 = 7.0 nM 8.15
CHEMBL5542885 EC50 = 11.0 nM 7.96
CHEMBL3545185 SELINEXOR EC50 = 12.0 nM 7.92
CHEMBL5566091 EC50 = 13.0 nM 7.89
CHEMBL5560534 EC50 = 19.0 nM 7.72
CHEMBL5564554 EC50 = 21.0 nM 7.68
CHEMBL5563530 EC50 = 23.0 nM 7.64
CHEMBL3545187 VERDINEXOR EC50 = 24.0 nM 7.62
CHEMBL5562376 EC50 = 24.0 nM 7.62
CHEMBL5542505 EC50 = 25.0 nM 7.60
CHEMBL5542934 EC50 = 26.0 nM 7.58
CHEMBL5561373 EC50 = 40.0 nM 7.40
CHEMBL130837 EC50 = 48.0 nM 7.32
CHEMBL5556828 EC50 = 55.0 nM 7.26
CHEMBL5563179 EC50 = 58.0 nM 7.24
CHEMBL5562296 EC50 = 65.0 nM 7.19
CHEMBL130007 EC50 = 82.0 nM 7.09
CHEMBL5566432 EC50 = 84.0 nM 7.08
CHEMBL5564519 EC50 = 91.0 nM 7.04
CHEMBL336546 EC50 = 106.0 nM 6.97
CHEMBL5566341 EC50 = 137.0 nM 6.86
CHEMBL5555764 EC50 = 137.0 nM 6.86
CHEMBL5561263 EC50 = 146.0 nM 6.84
CHEMBL5560350 EC50 = 206.0 nM 6.69
CHEMBL5565311 EC50 = 261.0 nM 6.58
CHEMBL5567104 EC50 = 358.0 nM 6.45
CHEMBL5563366 EC50 = 404.0 nM 6.39
CHEMBL5567882 EC50 = 501.0 nM 6.30
CHEMBL5561442 EC50 = 856.0 nM 6.07
CHEMBL5562070 EC50 = 913.0 nM 6.04
CHEMBL5568216 EC50 = 1334.0 nM 5.88
CHEMBL5561311 EC50 = 1396.0 nM 5.86
CHEMBL424086 EC50 = 1405.0 nM 5.85
CHEMBL5563183 EC50 = 1646.0 nM 5.78
CHEMBL5561264 EC50 = 2642.0 nM 5.58
CHEMBL132495 EC50 = 4090.0 nM 5.39
CHEMBL5558576 EC50 = 5406.0 nM 5.27
CHEMBL5564418 EC50 = 6690.0 nM 5.17
CHEMBL5563692 EC50 = 8123.0 nM 5.09
CHEMBL5560389 EC50 > 10000.0 nM -