Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1764697

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

Binding
Inhibition of IGF-induced autophosphosphorylation of GST-tagged human IGF1R expressed in SF21 cells after 10 mins by time resolved-fluorescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
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 5 6.83 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762179 1 7.04
CHEMBL1762178 1 7.01
CHEMBL1762177 1 6.81
CHEMBL1762176 1 6.70
CHEMBL1762155 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762179 IC50 = 92.0 nM 7.04
CHEMBL1762178 IC50 = 98.0 nM 7.01
CHEMBL1762177 IC50 = 154.0 nM 6.81
CHEMBL1762176 IC50 = 202.0 nM 6.70
CHEMBL1762155 IC50 = 264.0 nM 6.58