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Assay Detail

CHEMBL881279

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

Binding
In vitro inhibitory concentration against IGF-1R kinase
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D.
J Med Chem (2005) 48 : 5639 -5643
PubMed 16134929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.88 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401930 1 7.00
CHEMBL231306 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401930 IC50 = 100.0 nM 7.00
CHEMBL231306 IC50 = 180.0 nM 6.75