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Assay Detail

CHEMBL5531847

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

Binding
Inhibition of His-tagged human recombinant wild type RET M918T mutant expressed in Sf9 cells using poly(Glu, Tyr) peptide as substrate in presence of ATP preincubated fo4 30 mins followed by substrate addition and measured after 1 hr by FRET analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
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

Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations.
Wang ZX, Li QQ, Cai J, Wu JZ, Wang JJ, Zhang MY, Wang QX, Tong ZJ, Yang J, Wei TH, Zhou Y, Dai WC, Ding N, Leng XJ, Sun SL, Xue X, Yu YC, Yang Y, Li NG, Shi ZH.
J Med Chem (2024) 67 : 4346 -4375
PubMed 38484122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.40 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4582651 PRALSETINIB 4.0 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4582651 PRALSETINIB IC50 = 0.4 nM 9.40