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Assay Detail

CHEMBL3789674

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

Binding
Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, Jeay S.
Bioorg Med Chem Lett (2016) 26 : 2057 -2064
PubMed 26951753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.61 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786100 1 8.14
CHEMBL1091644 LINSITINIB 3.0 1 8.12
CHEMBL3787271 1 8.11
CHEMBL3787567 1 7.96
CHEMBL3787614 1 7.92
CHEMBL3785500 1 7.85
CHEMBL3786167 1 7.82
CHEMBL3785951 1 7.80
CHEMBL3787636 1 7.80
CHEMBL1614712 1 7.70
CHEMBL3786634 1 7.68
CHEMBL3787436 1 7.57
CHEMBL3786558 1 7.54
CHEMBL3786149 1 7.33
CHEMBL3787630 1 7.04
CHEMBL3786153 1 6.60
CHEMBL3787112 1 6.34
CHEMBL3785995 1 -
CHEMBL3785425 1 -
CHEMBL3786326 1 -
CHEMBL3786025 1 -
CHEMBL3785376 1 -
CHEMBL3787360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786100 IC50 = 7.3 nM 8.14
CHEMBL1091644 LINSITINIB IC50 = 7.6 nM 8.12
CHEMBL3787271 IC50 = 7.8 nM 8.11
CHEMBL3787567 IC50 = 11.0 nM 7.96
CHEMBL3787614 IC50 = 12.0 nM 7.92
CHEMBL3785500 IC50 = 14.0 nM 7.85
CHEMBL3786167 IC50 = 15.0 nM 7.82
CHEMBL3785951 IC50 = 16.0 nM 7.80
CHEMBL3787636 IC50 = 16.0 nM 7.80
CHEMBL1614712 IC50 = 20.0 nM 7.70
CHEMBL3786634 IC50 = 21.0 nM 7.68
CHEMBL3787436 IC50 = 27.0 nM 7.57
CHEMBL3786558 IC50 = 29.0 nM 7.54
CHEMBL3786149 IC50 = 47.0 nM 7.33
CHEMBL3787630 IC50 = 92.0 nM 7.04
CHEMBL3786153 IC50 = 251.0 nM 6.60
CHEMBL3787112 IC50 = 454.0 nM 6.34
CHEMBL3785995 IC50 - -
CHEMBL3785425 IC50 - -
CHEMBL3786326 IC50 - -
CHEMBL3786025 IC50 - -
CHEMBL3785376 IC50 < 4.6 nM -
CHEMBL3787360 IC50 - -