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Assay Detail

CHEMBL1228261

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

Binding
Inhibition of IGF1R in IGF1R-SAL cells
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IGF1R-SAL
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.
Sampognaro AJ, Wittman MD, Carboni JM, Chang C, Greer AF, Hurlburt WW, Sack JS, Vyas DM.
Bioorg Med Chem Lett (2010) 20 : 5027 -5030
PubMed 20675137 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1222709 1 9.00
CHEMBL575448 BMS-754807 2.0 1 8.68
CHEMBL1222855 1 7.40
CHEMBL1222710 1 6.79
CHEMBL1222791 2 6.69
CHEMBL1222792 1 6.62
CHEMBL1222790 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1222709 IC50 = 1.0 nM 9.00
CHEMBL575448 BMS-754807 IC50 = 2.1 nM 8.68
CHEMBL1222855 IC50 = 40.0 nM 7.40
CHEMBL1222710 IC50 = 162.0 nM 6.79
CHEMBL1222791 IC50 = 206.0 nM 6.69
CHEMBL1222792 IC50 = 237.0 nM 6.62
CHEMBL1222791 IC50 = 389.0 nM 6.41
CHEMBL1222790 IC50 = 508.0 nM 6.29