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Assay Detail

CHEMBL5615232

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 tagged mouse recombinant EphA2 (Ala22 to Ala535 residues) preincubated for 1 hr followed by ephrin-A1-Fc addition and measured after 4 to 5 hrs by ELISA assay
19
Total Activities
19
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
IC50 19 5.00 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5619189 1 5.58
CHEMBL5618209 1 5.44
CHEMBL5619481 1 5.33
CHEMBL3735992 1 5.27
CHEMBL5618680 1 5.26
CHEMBL5620271 1 5.25
CHEMBL5619502 1 5.16
CHEMBL5619796 1 5.09
CHEMBL5620315 1 5.09
CHEMBL5618992 1 5.08
CHEMBL5619612 1 5.00
CHEMBL5620294 1 4.92
CHEMBL5620153 1 4.80
CHEMBL5618293 1 4.80
CHEMBL5618286 1 4.70
CHEMBL5620004 1 4.62
CHEMBL5619360 1 4.62
CHEMBL5620093 1 4.54
CHEMBL5618542 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5619189 IC50 = 2600.0 nM 5.58
CHEMBL5618209 IC50 = 3600.0 nM 5.44
CHEMBL5619481 IC50 = 4700.0 nM 5.33
CHEMBL3735992 IC50 = 5400.0 nM 5.27
CHEMBL5618680 IC50 = 5500.0 nM 5.26
CHEMBL5620271 IC50 = 5600.0 nM 5.25
CHEMBL5619502 IC50 = 6900.0 nM 5.16
CHEMBL5619796 IC50 = 8100.0 nM 5.09
CHEMBL5620315 IC50 = 8200.0 nM 5.09
CHEMBL5618992 IC50 = 8300.0 nM 5.08
CHEMBL5619612 IC50 = 9900.0 nM 5.00
CHEMBL5620294 IC50 = 12000.0 nM 4.92
CHEMBL5620153 IC50 = 16000.0 nM 4.80
CHEMBL5618293 IC50 = 16000.0 nM 4.80
CHEMBL5618286 IC50 = 20000.0 nM 4.70
CHEMBL5620004 IC50 = 24000.0 nM 4.62
CHEMBL5619360 IC50 = 24000.0 nM 4.62
CHEMBL5620093 IC50 = 29000.0 nM 4.54
CHEMBL5618542 IC50 = 38000.0 nM 4.42