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Assay Detail

CHEMBL3790306

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

Binding
Inhibition of RET (unknown origin) in presence of [gamma33P]ATP
6
Total Activities
6
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

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, Jeay S.
Bioorg Med Chem Lett (2016) 26 : 2057 -2064
PubMed 26951753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.84 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787112 1 8.10
CHEMBL1614712 1 5.48
CHEMBL3787614 1 5.36
CHEMBL3785951 1 5.22
CHEMBL3786167 1 5.03
CHEMBL3785500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787112 IC50 = 8.0 nM 8.10
CHEMBL1614712 IC50 = 3300.0 nM 5.48
CHEMBL3787614 IC50 = 4400.0 nM 5.36
CHEMBL3785951 IC50 = 6000.0 nM 5.22
CHEMBL3786167 IC50 = 9300.0 nM 5.03
CHEMBL3785500 IC50 > 10000.0 nM -