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Assay Detail

CHEMBL4359465

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

Binding
Inhibition of human ERG expressed in HEK293 cells by patch clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.
Moccia M, Frett B, Zhang L, Lakkaniga NR, Briggs DC, Chauhan R, Brescia A, Federico G, Yan W, Santoro M, McDonald NQ, Li HY, Carlomagno F.
J Med Chem (2020) 63 : 4506 -4516
PubMed 32298114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.35 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327980 1 7.57
CHEMBL4473213 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327980 IC50 = 27.0 nM 7.57
CHEMBL4473213 IC50 = 7570.0 nM 5.12