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Assay Detail

CHEMBL4359520

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

Binding
Inhibition of RET isoform 9 C634W mutant in human TT cells assessed as reduction in cell proliferation supplemented with fresh medium containing compound for every 2 to 3 days and measured during compound dosing
1
Total Activities
1
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

Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041)
Type SINGLE PROTEIN
Organism Homo sapiens

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 1 9.17 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4473213 1 9.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4473213 IC50 = 0.67 nM 9.17