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Assay Detail

CHEMBL5615243

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

Binding
Displacement of biotinylated Fc-tagged ephrin-A1 from C/N-terminal 6-His tag mouse recombinant EphA2 (Ala22 to Ala535 residues) assessed as inhibition constant 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 Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ephrin type-A receptor 2 (CHEMBL4105859)
Type SINGLE PROTEIN
Organism Mus musculus

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
Ki 3 5.69 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735992 1 5.85
CHEMBL5619796 1 5.66
CHEMBL5619189 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735992 Ki = 1400.0 nM 5.85
CHEMBL5619796 Ki = 2200.0 nM 5.66
CHEMBL5619189 Ki = 2800.0 nM 5.55