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Assay Detail

CHEMBL4231192

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

Binding
Inhibition of recombinant human RET V804L mutant using peptide as substrate by fluorimetric analysis
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 Intermediate

Target

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

Publication

Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
La Pietra V, Sartini S, Botta L, Antonelli A, Ferrari SM, Fallahi P, Moriconi A, Coviello V, Quattrini L, Ke YY, Hsing-Pang H, Da Settimo F, Novellino E, La Motta C, Marinelli L.
Eur J Med Chem (2018) 150 : 491 -505
PubMed 29549836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.59 4.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4238771 1 4.99
CHEMBL1488812 1 4.18
CHEMBL47173 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4238771 IC50 = 10300.0 nM 4.99
CHEMBL1488812 IC50 = 66200.0 nM 4.18
CHEMBL47173 IC50 - -