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Assay Detail

CHEMBL1764694

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

Binding
Inhibition of autophosphosphorylation of human IGF1R expressed in IGF1-stimulated MCF7 cells by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Insulin-like growth factor 1 receptor (CHEMBL1957)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.
Lesuisse D, Mauger J, Nemecek C, Maignan S, Boiziau J, Harlow G, Hittinger A, Ruf S, Strobel H, Nair A, Ritter K, Malleron JL, Dagallier A, El-Ahmad Y, Guilloteau JP, Guizani H, Bouchard H, Venot C.
Bioorg Med Chem Lett (2011) 21 : 2224 -2228
PubMed 21441024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.19 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762178 1 8.15
CHEMBL1762179 1 7.47
CHEMBL1762176 1 7.37
CHEMBL1762177 1 7.33
CHEMBL1762155 1 6.93
CHEMBL1762148 1 6.84
CHEMBL1738841 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762178 IC50 = 7.0 nM 8.15
CHEMBL1762179 IC50 = 34.0 nM 7.47
CHEMBL1762176 IC50 = 43.0 nM 7.37
CHEMBL1762177 IC50 = 47.0 nM 7.33
CHEMBL1762155 IC50 = 117.0 nM 6.93
CHEMBL1762148 IC50 = 145.0 nM 6.84
CHEMBL1738841 IC50 = 600.0 nM 6.22