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Assay Detail

CHEMBL5151901

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

Binding
Inhibition of RET (unknown origin)
3
Total Activities
3
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

Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.
Saha D, Ryan KR, Lakkaniga NR, Acharya B, Garcia NG, Smith EL, Frett B.
J Med Chem (2021) 64 : 11747 -11773
PubMed 34402300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.81 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24828 VANDETANIB 4.0 1 9.89
CHEMBL535 SUNITINIB 4.0 1 8.30
CHEMBL1336 SORAFENIB 4.0 1 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24828 VANDETANIB IC50 = 0.13 nM 9.89
CHEMBL535 SUNITINIB IC50 = 5.0 nM 8.30
CHEMBL1336 SORAFENIB IC50 = 5.9 nM 8.23