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Assay Detail

CHEMBL1785336

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

Binding
Inhibition of human RET using KKKSPGEYVNIEFG by Hotspot assay
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

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC.
Bioorg Med Chem Lett (2011) 21 : 3743 -3748
PubMed 21561767 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1784637 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1784637 IC50 = 0.2 nM 9.70