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Assay Detail

CHEMBL887273

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Functional
Inhibition of IGF1R expressed in Sal cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Sal
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
Wittman MD, Balasubramanian B, Stoffan K, Velaparthi U, Liu P, Krishnanathan S, Carboni J, Li A, Greer A, Attar R, Gottardis M, Chang C, Jacobson B, Sun Y, Hansel S, Zoeckler M, Vyas DM.
Bioorg Med Chem Lett (2007) 17 : 974 -977
PubMed 17187980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.14 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389605 1 6.72
CHEMBL231306 1 6.43
CHEMBL230902 1 6.38
CHEMBL425303 1 6.36
CHEMBL231305 1 6.33
CHEMBL390198 1 6.27
CHEMBL231110 1 6.21
CHEMBL231212 1 6.12
CHEMBL231004 1 6.12
CHEMBL231003 1 6.11
CHEMBL231002 1 6.11
CHEMBL231112 1 5.90
CHEMBL231407 1 5.79
CHEMBL231311 1 5.75
CHEMBL388206 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389605 IC50 = 190.0 nM 6.72
CHEMBL231306 IC50 = 370.0 nM 6.43
CHEMBL230902 IC50 = 420.0 nM 6.38
CHEMBL425303 IC50 = 440.0 nM 6.36
CHEMBL231305 IC50 = 470.0 nM 6.33
CHEMBL390198 IC50 = 540.0 nM 6.27
CHEMBL231110 IC50 = 610.0 nM 6.21
CHEMBL231212 IC50 = 760.0 nM 6.12
CHEMBL231004 IC50 = 750.0 nM 6.12
CHEMBL231003 IC50 = 780.0 nM 6.11
CHEMBL231002 IC50 = 780.0 nM 6.11
CHEMBL231112 IC50 = 1270.0 nM 5.90
CHEMBL231407 IC50 = 1640.0 nM 5.79
CHEMBL231311 IC50 = 1790.0 nM 5.75
CHEMBL388206 IC50 = 3630.0 nM 5.44