Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1108832

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

Binding
Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Fidanze SD, Erickson SA, Wang GT, Mantei R, Clark RF, Sorensen BK, Bamaung NY, Kovar P, Johnson EF, Swinger KK, Stewart KD, Zhang Q, Tucker LA, Pappano WN, Wilsbacher JL, Wang J, Sheppard GS, Bell RL, Davidsen SK, Hubbard RD.
Bioorg Med Chem Lett (2010) 20 : 2452 -2455
PubMed 20346655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.56 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1090364 1 7.57
CHEMBL1090363 1 7.34
CHEMBL1090362 1 7.28
CHEMBL1090361 1 7.09
CHEMBL1090359 1 7.00
CHEMBL1090356 1 6.89
CHEMBL1090357 1 6.68
CHEMBL1090358 1 6.64
CHEMBL1090360 1 6.55
CHEMBL1090355 1 6.35
CHEMBL1090353 1 6.24
CHEMBL1090354 1 6.23
CHEMBL1090352 1 5.96
CHEMBL1090351 1 5.89
CHEMBL1090350 1 5.82
CHEMBL1088931 1 5.42
CHEMBL1093486 1 -
CHEMBL1093235 1 -
CHEMBL1093234 1 -
CHEMBL1093815 1 -
CHEMBL1091613 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1090364 IC50 = 27.0 nM 7.57
CHEMBL1090363 IC50 = 46.0 nM 7.34
CHEMBL1090362 IC50 = 52.0 nM 7.28
CHEMBL1090361 IC50 = 81.0 nM 7.09
CHEMBL1090359 IC50 = 100.0 nM 7.00
CHEMBL1090356 IC50 = 130.0 nM 6.89
CHEMBL1090357 IC50 = 210.0 nM 6.68
CHEMBL1090358 IC50 = 230.0 nM 6.64
CHEMBL1090360 IC50 = 280.0 nM 6.55
CHEMBL1090355 IC50 = 450.0 nM 6.35
CHEMBL1090353 IC50 = 580.0 nM 6.24
CHEMBL1090354 IC50 = 590.0 nM 6.23
CHEMBL1090352 IC50 = 1100.0 nM 5.96
CHEMBL1090351 IC50 = 1300.0 nM 5.89
CHEMBL1090350 IC50 = 1500.0 nM 5.82
CHEMBL1088931 IC50 = 3800.0 nM 5.42
CHEMBL1093486 IC50 > 12500.0 nM -
CHEMBL1093235 IC50 > 12500.0 nM -
CHEMBL1093234 IC50 > 12500.0 nM -
CHEMBL1093815 IC50 > 12500.0 nM -
CHEMBL1091613 IC50 > 12500.0 nM -