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Assay Detail

CHEMBL5615233

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

Binding
Displacement of biotinylated Fc-tagged ephrin-A1 from N/C-terminal 6-his tagged human recombinant EphA1 (Lys26 to Glu547 residues) preincubated for 1 hr followed by ephrin-A1-Fc addition and measured after 4 to 5 hrs by ELISA assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ephrin type-A receptor 1 (CHEMBL5810)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new 1-(phenylsulfonyl)-1H-indole derivative targeting the EphA2 receptor with antiproliferative activity on U251 glioblastoma cell line.
Guidetti L, Castelli R, Zappia A, Ferrari FR, Giorgio C, Barocelli E, Pagliaro L, Vento F, Roti G, Scalvini L, Vacondio F, Rivara S, Mor M, Lodola A, Tognolini M.
Eur J Med Chem (2024) 276 : 116681 -116681
PubMed 39024966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.19 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735992 1 5.66
CHEMBL5619796 1 4.96
CHEMBL5619189 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735992 IC50 = 2200.0 nM 5.66
CHEMBL5619796 IC50 = 11000.0 nM 4.96
CHEMBL5619189 IC50 = 11000.0 nM 4.96