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Assay Detail

CHEMBL5650783

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

Binding
Inhibition of Nano Luc-fused full length C-terminal EPHA3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ephrin type-A receptor 3 (CHEMBL4954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Tröster A, Heinzlmeir S, Berger BT, Gande SL, Saxena K, Sreeramulu S, Linhard V, Nasiri AH, Bolte M, Müller S, Kuster B, Médard G, Kudlinzki D, Schwalbe H.
ChemMedChem (2018) 13 : 1629 -1633
PubMed 29928781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.78 9.52

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752910 1 9.52
CHEMBL1421 DASATINIB ANHYDROUS 4.0 1 9.52
CHEMBL5653589 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752910 IC50 = 0.3 nM 9.52
CHEMBL1421 DASATINIB ANHYDROUS IC50 = 0.3 nM 9.52
CHEMBL5653589 IC50 = 50.0 nM 7.30