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Compound Detail

CHEMBL4634073

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COC(=O)Nc1ccc(-c2c(OC3CCN(C)CC3)nc3c(-c4ccc(OC)c(OC)c4)cnn3c2N)cc1

Basic Information

ChEMBL ID CHEMBL4634073
Phase Preclinical
Structure Type MOL
InChI Key UKYJKXMPIDEQFF-UHFFFAOYSA-N
31
Targets
32
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

532.6
MW (Da)
4.31
ALogP
10
HBA
2
HBD
125.5
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N6O5
MW 532.60
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.89

Activity Summary

IC50 32 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 8.22 8.22 6.0 1
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET
CHEMBL3430888
IC50 8.22 7.97 6.0 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.1 8.1 8.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.0 8.0 10.0 1
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 7.77 7.77 17.0 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.7 7.7 20.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 7.66 7.66 22.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.58 7.58 26.0 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.46 7.46 35.0 1
Tyrosine-protein kinase Lyn
CHEMBL3905
IC50 7.17 7.17 67.0 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 7.09 7.09 82.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 7.08 7.08 84.0 1
Tyrosine-protein kinase Mer
CHEMBL5331
IC50 7.07 7.07 86.0 1
Tyrosine-protein kinase Blk
CHEMBL2250
IC50 6.64 6.64 230.0 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 6.37 6.37 430.0 1
Tyrosine-protein kinase Fgr
CHEMBL4454
IC50 6.36 6.36 440.0 1
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor)
CHEMBL2111387
IC50 5.92 5.92 1200.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 5.85 5.85 1400.0 1
NT-3 growth factor receptor
CHEMBL5608
IC50 5.85 5.85 1400.0 1
BDNF/NT-3 growth factors receptor
CHEMBL4898
IC50 5.68 5.68 2100.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 5.62 5.62 2400.0 1
High affinity nerve growth factor receptor
CHEMBL2815
IC50 5.55 5.55 2800.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 5.52 5.52 3000.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.47 5.47 3400.0 1
Tyrosine-protein kinase receptor TYRO3
CHEMBL5314
IC50 5.43 5.43 3700.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 5.3 5.3 5000.0 1
BaF3
CHEMBL614524
IC50 5.3 5.3 5000.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 5.29 5.29 5100.0 1
Proto-oncogene tyrosine-protein kinase ROS
CHEMBL5568
IC50 5.26 5.26 5500.0 1
Macrophage-stimulating protein receptor
CHEMBL2689
IC50 5.22 5.22 6000.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 5.04 5.04 9100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 6.0 nM 8.22 Inhibition of RET (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET IC50 = 6.0 nM 8.22 Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assess... 32292564
Fibroblast growth factor receptor 2 IC50 = 8.0 nM 8.1 Inhibition of FGFR2 (unknown origin) transfected in mouse Ba/F3 cells assessed a... 32292564
Fibroblast growth factor receptor 1 IC50 = 10.0 nM 8.0 Inhibition of FGFR1 (unknown origin) transfected in mouse Ba/F3 cells assessed a... 32292564
Platelet-derived growth factor receptor alpha IC50 = 17.0 nM 7.77 Inhibition of PDGFRalpha (unknown origin) transfected in mouse Ba/F3 cells asses... 32292564
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET IC50 = 19.0 nM 7.72 Inhibition of KIF5B-RET V804M mutant (unknown origin) transfected in mouse Ba/F3... 32292564
Mast/stem cell growth factor receptor Kit IC50 = 20.0 nM 7.7 Inhibition of KIT (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Platelet-derived growth factor receptor beta IC50 = 22.0 nM 7.66 Inhibition of PDGFRbeta (unknown origin) transfected in mouse Ba/F3 cells assess... 32292564
Vascular endothelial growth factor receptor 2 IC50 = 26.0 nM 7.58 Inhibition of KDR (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Fibroblast growth factor receptor 4 IC50 = 35.0 nM 7.46 Inhibition of FGFR4 (unknown origin) transfected in mouse Ba/F3 cells assessed a... 32292564
Tyrosine-protein kinase Lyn IC50 = 67.0 nM 7.17 Inhibition of LYN (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Macrophage colony-stimulating factor 1 receptor IC50 = 82.0 nM 7.09 Inhibition of FMS (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Tyrosine-protein kinase JAK2 IC50 = 84.0 nM 7.08 Inhibition of JAK2 (unknown origin) transfected in mouse Ba/F3 cells assessed as... 32292564
Tyrosine-protein kinase Mer IC50 = 86.0 nM 7.07 Inhibition of MER (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Tyrosine-protein kinase Blk IC50 = 230.0 nM 6.64 Inhibition of BLK (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
Fibroblast growth factor receptor 3 IC50 = 430.0 nM 6.37 Inhibition of FGFR3 (unknown origin) transfected in mouse Ba/F3 cells assessed a... 32292564
Tyrosine-protein kinase Fgr IC50 = 440.0 nM 6.36 Inhibition of FGR (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) IC50 = 1200.0 nM 5.92 Inhibition of NPM/ALK (unknown origin) transfected in mouse Ba/F3 cells assessed... 32292564
Tyrosine-protein kinase SYK IC50 = 1400.0 nM 5.85 Inhibition of SYK (unknown origin) transfected in mouse Ba/F3 cells assessed as ... 32292564
NT-3 growth factor receptor IC50 = 1400.0 nM 5.85 Inhibition of TRKC (unknown origin) transfected in mouse Ba/F3 cells assessed as... 32292564

Literature References

PubMed DOI Target Context # Activities
32292564 10.1021/acsmedchemlett.0c00015 Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET 2
32292564 10.1021/acsmedchemlett.0c00015 Tyrosine-protein kinase ZAP-70 1
32292564 10.1021/acsmedchemlett.0c00015 BaF3 1
32292564 10.1021/acsmedchemlett.0c00015 Mast/stem cell growth factor receptor Kit 1
32292564 10.1021/acsmedchemlett.0c00015 Vascular endothelial growth factor receptor 2 1
32292564 10.1021/acsmedchemlett.0c00015 Tyrosine-protein kinase JAK2 1
32292564 10.1021/acsmedchemlett.0c00015 Insulin receptor 1
32292564 10.1021/acsmedchemlett.0c00015 Insulin-like growth factor 1 receptor 1
32292564 10.1021/acsmedchemlett.0c00015 Macrophage colony-stimulating factor 1 receptor 1
32292564 10.1021/acsmedchemlett.0c00015 Receptor-type tyrosine-protein kinase FLT3 1
32292564 10.1021/acsmedchemlett.0c00015 Vascular endothelial growth factor receptor 1 1
32292564 10.1021/acsmedchemlett.0c00015 Tyrosine-protein kinase Fgr 1
32292564 10.1021/acsmedchemlett.0c00015 Fibroblast growth factor receptor 4 1
32292564 10.1021/acsmedchemlett.0c00015 Fibroblast growth factor receptor 3 1
32292564 10.1021/acsmedchemlett.0c00015 Fibroblast growth factor receptor 2 1
32292564 10.1021/acsmedchemlett.0c00015 Fibroblast growth factor receptor 1 1
32292564 10.1021/acsmedchemlett.0c00015 Cytoplasmic tyrosine-protein kinase BMX 1
32292564 10.1021/acsmedchemlett.0c00015 Tyrosine-protein kinase Blk 1
32292564 10.1021/acsmedchemlett.0c00015 NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) 1
32292564 10.1021/acsmedchemlett.0c00015 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine