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Assay Detail

CHEMBL827789

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

Binding
Inhibition of insulin Receptor kinase
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Insulin receptor (CHEMBL1981)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.
J Med Chem (2005) 48 : 4892 -4909
PubMed 16033269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.39 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177688 1 5.77
CHEMBL188502 1 5.00
CHEMBL372657 1 -
CHEMBL188386 1 -
CHEMBL190984 1 -
CHEMBL371169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177688 IC50 = 1690.0 nM 5.77
CHEMBL188502 IC50 = 10000.0 nM 5.00
CHEMBL372657 IC50 > 10000.0 nM -
CHEMBL188386 IC50 > 10000.0 nM -
CHEMBL190984 IC50 > 10000.0 nM -
CHEMBL371169 IC50 > 10000.0 nM -