Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3738294

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

Binding
Displacement of biotinylated-ephrin-A1-Fc from EphA2-Fc receptor (unknown origin) preincubated for 1 hr followed by biotinylated-ephrin-A1-Fc addition measured after 4 hrs by ELISA
15
Total Activities
15
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 2 (CHEMBL2068)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
Castelli R, Tognolini M, Vacondio F, Incerti M, Pala D, Callegari D, Bertoni S, Giorgio C, Hassan-Mohamed I, Zanotti I, Bugatti A, Rusnati M, Festuccia C, Rivara S, Barocelli E, Mor M, Lodola A.
Eur J Med Chem (2015) 103 : 312 -324
PubMed 26363867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.89 5.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3734863 1 5.45
CHEMBL3736250 1 5.39
CHEMBL3735992 1 5.37
CHEMBL3734937 1 5.30
CHEMBL3735509 1 5.22
CHEMBL3736171 1 5.20
CHEMBL3736070 1 5.05
CHEMBL3736176 1 4.65
CHEMBL169264 1 4.40
CHEMBL3736217 1 4.32
CHEMBL3735472 1 4.30
CHEMBL3736006 1 4.05
CHEMBL3736288 1 -
CHEMBL3735198 1 -
CHEMBL3734875 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3734863 IC50 = 3548.13 nM 5.45
CHEMBL3736250 IC50 = 4073.8 nM 5.39
CHEMBL3735992 IC50 = 4265.8 nM 5.37
CHEMBL3734937 IC50 = 5011.87 nM 5.30
CHEMBL3735509 IC50 = 6025.6 nM 5.22
CHEMBL3736171 IC50 = 6309.57 nM 5.20
CHEMBL3736070 IC50 = 8912.51 nM 5.05
CHEMBL3736176 IC50 = 22387.21 nM 4.65
CHEMBL169264 IC50 = 39810.72 nM 4.40
CHEMBL3736217 IC50 = 47863.01 nM 4.32
CHEMBL3735472 IC50 = 50118.72 nM 4.30
CHEMBL3736006 IC50 = 89125.09 nM 4.05
CHEMBL3736288 IC50 > 100000.0 nM -
CHEMBL3735198 IC50 > 100000.0 nM -
CHEMBL3734875 IC50 > 100000.0 nM -