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Assay Detail

CHEMBL5679224

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

Binding
Inhibition of human IR autophosphorylation in insulin- stimulated mouse NIH-3T3-hIR cells pre incubated for 6 hr followed by insulin stimulation and measured after 15 mins by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH-3T3-hIR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Insulin receptor (CHEMBL1981)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R.
Clin Cancer Res (2009) 15 : 3058 -3067
PubMed 19383820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.72 7.72

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL466397 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL466397 IC50 = 19.0 nM 7.72