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Assay Detail

CHEMBL5679221

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

Binding
Inhibition of intracellular domain of GST-tagged IGF1R (957 to 1367 residues) (unknown origin) expressed in baculovirus expression system using biotin-aminohexyl-AEEEEYMMMMAKKKK-NH2 as substrate pre incubated for 6 hrs followed by substrate addition and measured after 2 hrs in presence of [gamma-33P]-ATP by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

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

Target

Insulin-like growth factor 1 receptor (CHEMBL1957)
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
Ki 1 8.80 8.80

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 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL466397 Ki = 1.6 nM 8.80