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Assay Detail

CHEMBL4003653

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

Binding
Displacement of biotinylated ephrin-A1-Fc from recombinant mouse EphA2 receptor preincubated for 1 hr followed by biotinylated ephrin-A1-Fc addition measured after 4 hrs by ELISA method
23
Total Activities
17
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

Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
Incerti M, Russo S, Callegari D, Pala D, Giorgio C, Zanotti I, Barocelli E, Vicini P, Vacondio F, Rivara S, Castelli R, Tognolini M, Lodola A.
J Med Chem (2017) 60 : 787 -796
PubMed 28005388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.01 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078429 2 6.10
CHEMBL3735125 2 6.04
CHEMBL4079387 2 5.75
CHEMBL4087778 1 5.51
CHEMBL4089696 1 5.41
CHEMBL4087107 1 5.00
CHEMBL4090681 1 4.89
CHEMBL4099159 1 4.85
CHEMBL4071291 1 4.77
CHEMBL4081123 1 4.75
CHEMBL4098329 2 4.58
CHEMBL4081825 1 4.55
CHEMBL4059908 2 4.55
CHEMBL4064652 2 4.54
CHEMBL408701 TAUROLITHOCHOLIC ACID 3.0 1 4.14
CHEMBL1478 LITHOCHOLIC ACID 1 4.10
CHEMBL4074295 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078429 IC50 = 794.33 nM 6.10
CHEMBL4078429 IC50 = 800.0 nM 6.10
CHEMBL3735125 IC50 = 912.01 nM 6.04
CHEMBL3735125 IC50 = 910.0 nM 6.04
CHEMBL4079387 IC50 = 1800.0 nM 5.75
CHEMBL4079387 IC50 = 1819.7 nM 5.74
CHEMBL4087778 IC50 = 3100.0 nM 5.51
CHEMBL4089696 IC50 = 3900.0 nM 5.41
CHEMBL4087107 IC50 = 10000.0 nM 5.00
CHEMBL4090681 IC50 = 13000.0 nM 4.89
CHEMBL4099159 IC50 = 14000.0 nM 4.85
CHEMBL4071291 IC50 = 17000.0 nM 4.77
CHEMBL4081123 IC50 = 18000.0 nM 4.75
CHEMBL4098329 IC50 = 26000.0 nM 4.58
CHEMBL4098329 IC50 = 26302.68 nM 4.58
CHEMBL4059908 IC50 = 28000.0 nM 4.55
CHEMBL4059908 IC50 = 28183.83 nM 4.55
CHEMBL4081825 IC50 = 28000.0 nM 4.55
CHEMBL4064652 IC50 = 29000.0 nM 4.54
CHEMBL4064652 IC50 = 28840.32 nM 4.54
CHEMBL408701 TAUROLITHOCHOLIC ACID IC50 = 72000.0 nM 4.14
CHEMBL1478 LITHOCHOLIC ACID IC50 = 79000.0 nM 4.10
CHEMBL4074295 IC50 = 83000.0 nM 4.08