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Assay Detail

CHEMBL4024845

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

Binding
Inhibition of CRM1-mediated nucleocytoplasmic transport in human HeLa cells after 90 mins by immunofluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.
Jackson PA, Widen JC, Harki DA, Brummond KM.
J Med Chem (2017) 60 : 839 -885
PubMed 27996267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.20 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486133 LEPTOMYCIN B 1 9.00
CHEMBL4088268 1 8.00
CHEMBL4077955 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486133 LEPTOMYCIN B IC50 = 1.0 nM 9.00
CHEMBL4088268 IC50 = 10.0 nM 8.00
CHEMBL4077955 IC50 = 25.0 nM 7.60