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Compound Detail

CHEMBL2037220

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CN1CCN(c2cc(C(=O)Nc3cccc(Nc4ccc5c(c4)NC(=O)/C5=C\c4cc(C(=O)O)c[nH]4)c3)cc(C(F)(F)F)c2)CC1

Basic Information

ChEMBL ID CHEMBL2037220
Phase Preclinical
Structure Type MOL
InChI Key FWZMHIPXROINAE-NTFVMDSBSA-N
15
Targets
18
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

630.6
MW (Da)
5.97
ALogP
6
HBA
5
HBD
129.8
PSA (Ų)
0.16
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H29F3N6O4
MW 630.63
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -1.15

Activity Summary

IC50 18 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 8.52 7.64 3.0 4
BDNF/NT-3 growth factors receptor
CHEMBL4898
IC50 7.77 7.77 17.0 1
Mast/stem cell growth factor receptor Kit
CHEMBL2034798
IC50 7.34 7.34 46.0 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2034799
IC50 7.0 7.0 100.0 1
Ephrin type-B receptor 2
CHEMBL5961
IC50 5.64 5.64 2300.0 1
Vascular endothelial growth factor receptor 1
CHEMBL3516
IC50 5.5 5.5 3200.0 1
Ephrin type-A receptor 3
CHEMBL2034794
IC50 5.27 5.27 5400.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL2034796
IC50 5.26 5.26 5500.0 1
Mitogen-activated protein kinase 9
CHEMBL2034797
IC50 5.25 5.25 5600.0 1
Tyrosine-protein kinase Fgr
CHEMBL2034795
IC50 5.2 5.2 6300.0 1
Tyrosine-protein kinase receptor Tie-1
CHEMBL2034800
IC50 5.16 5.16 7000.0 1
Proto-oncogene tyrosine-protein kinase ROS
CHEMBL2034802
IC50 5.16 5.16 7000.0 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL5570
IC50 5.12 5.12 7600.0 1
Unchecked
CHEMBL612545
IC50 5.09 5.09 8200.0 1
ALK tyrosine kinase receptor
CHEMBL5771
IC50 5.06 5.06 8800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 3.0 nM 8.52 Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKB 24900443
NON-PROTEIN TARGET IC50 = 6.0 nM 8.22 Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC 24900443
NON-PROTEIN TARGET IC50 = 10.0 nM 8.0 Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKA 24900443
BDNF/NT-3 growth factors receptor IC50 = 17.0 nM 7.77 Inhibition of TRKB by HTRF assay 24900443
Mast/stem cell growth factor receptor Kit IC50 = 46.0 nM 7.34 Inhibition of Tel-fused KIT in mouse BA/F3 cells 24900443
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 100.0 nM 7.0 Inhibition of Tel-fused RET in mouse BA/F3 cells 24900443
NON-PROTEIN TARGET IC50 = 1500.0 nM 5.82 Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR 24900443
Ephrin type-B receptor 2 IC50 = 2300.0 nM 5.64 Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells 24900443
Vascular endothelial growth factor receptor 1 IC50 = 3200.0 nM 5.5 Inhibition of Tel-fused FLT1 in mouse BA/F3 cells 24900443
Ephrin type-A receptor 3 IC50 = 5400.0 nM 5.27 Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells 24900443
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5500.0 nM 5.26 Inhibition of Tel-fused FLT3 in mouse BA/F3 cells 24900443
Mitogen-activated protein kinase 9 IC50 = 5600.0 nM 5.25 Inhibition of Tel-fused JNK2 in mouse BA/F3 cells 24900443
Tyrosine-protein kinase Fgr IC50 = 6300.0 nM 5.2 Inhibition of Tel-fused FGR in mouse BA/F3 cells 24900443
Proto-oncogene tyrosine-protein kinase ROS IC50 = 7000.0 nM 5.16 Inhibition of Tel-fused ROS in mouse BA/F3 cells 24900443
Tyrosine-protein kinase receptor Tie-1 IC50 = 7000.0 nM 5.16 Inhibition of Tel-fused TIE1 in mouse BA/F3 cells 24900443
Macrophage colony-stimulating factor 1 receptor IC50 = 7600.0 nM 5.12 Inhibition of Tel-fused FMS in mouse BA/F3 cells 24900443
Unchecked IC50 = 8200.0 nM 5.09 Inhibition of Bcr-ABL in mouse BA/F3 cells 24900443
ALK tyrosine kinase receptor IC50 = 8800.0 nM 5.06 Inhibition of Tel-fused ALK in mouse BA/F3 cells 24900443

Literature References

PubMed DOI Target Context # Activities
24900443 10.1021/ml200261d NON-PROTEIN TARGET 4
24900443 10.1021/ml200261d Unchecked 2
24900443 10.1021/ml200261d Macrophage colony-stimulating factor 1 receptor 1
24900443 10.1021/ml200261d Cytoplasmic tyrosine-protein kinase BMX 1
24900443 10.1021/ml200261d Ephrin type-A receptor 3 1
24900443 10.1021/ml200261d Ephrin type-B receptor 2 1
24900443 10.1021/ml200261d Fibroblast growth factor receptor 3 1
24900443 10.1021/ml200261d Fibroblast growth factor receptor 4 1
24900443 10.1021/ml200261d Tyrosine-protein kinase Fgr 1
24900443 10.1021/ml200261d Vascular endothelial growth factor receptor 1 1
24900443 10.1021/ml200261d Receptor-type tyrosine-protein kinase FLT3 1
24900443 10.1021/ml200261d Proto-oncogene tyrosine-protein kinase ROS 1
24900443 10.1021/ml200261d Insulin-like growth factor 1 receptor 1
24900443 10.1021/ml200261d Insulin receptor 1
24900443 10.1021/ml200261d Mitogen-activated protein kinase 9 1
24900443 10.1021/ml200261d Mast/stem cell growth factor receptor Kit 1
24900443 10.1021/ml200261d Tyrosine-protein kinase Lyn 1
24900443 10.1021/ml200261d Proto-oncogene tyrosine-protein kinase receptor Ret 1
24900443 10.1021/ml200261d Macrophage-stimulating protein receptor 1
24900443 10.1021/ml200261d Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine