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Compound Detail

CHEMBL5598552

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CCN1CCN(c2ccc(NC(=O)Nc3ccc(-c4cc(C(=O)NC)c5ncccc5n4)cc3)cc2C(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL5598552
Phase Preclinical
Structure Type MOL
InChI Key URSBFSYPZGOCKS-UHFFFAOYSA-N
12
Targets
14
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

577.6
MW (Da)
5.46
ALogP
6
HBA
3
HBD
102.5
PSA (Ų)
0.28
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30F3N7O2
MW 577.61
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.67

Activity Summary

IC50 14 meas. best 7.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 7.13 6.71 73.9 3
BMDM
CHEMBL4296525
IC50 6.78 6.78 167.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.32 6.32 483.6 1
NT-3 growth factor receptor
CHEMBL5608
IC50 6.05 6.05 889.2 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 6.03 6.03 945.1 1
High affinity nerve growth factor receptor
CHEMBL2815
IC50 6.02 6.02 958.0 1
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 6.0 6.0 992.3 1
Hep 3B2
CHEMBL4296437
IC50 5.75 5.75 1790.0 1
HepG2
CHEMBL395
IC50 5.62 5.62 2370.0 1
HS27
CHEMBL614666
IC50 5.06 5.06 8800.0 1
WI-38
CHEMBL614391
IC50 4.78 4.78 16700.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.08 4.08 83450.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Macrophage colony-stimulating factor 1 receptor IC50 = 73.9 nM 7.13 Inhibition of FMS (unknown origin) using myelin basic protein as substrate measu... 38850857
Macrophage colony-stimulating factor 1 receptor IC50 = 74.13 nM 7.13 Inhibition of FMS (unknown origin) using myelin basic protein as substrate measu... 38850857
BMDM IC50 = 167.0 nM 6.78 Inhibition of CSF-1-induced C57BL6 mouse BMDM cell growth preincubated for 1 hr ... 38850857
Receptor-type tyrosine-protein kinase FLT3 IC50 = 483.6 nM 6.32 Inhibition of FLT3 (unknown origin) using myelin basic protein as substrate meas... 38850857
NT-3 growth factor receptor IC50 = 889.2 nM 6.05 Inhibition of TrkC (unknown origin) using myelin basic protein as substrate meas... 38850857
Vascular endothelial growth factor receptor 3 IC50 = 945.1 nM 6.03 Inhibition of FLT4 (unknown origin) using myelin basic protein as substrate meas... 38850857
High affinity nerve growth factor receptor IC50 = 958.0 nM 6.02 Inhibition of TrkA (unknown origin) using myelin basic protein as substrate meas... 38850857
Platelet-derived growth factor receptor alpha IC50 = 992.3 nM 6.0 Inhibition of PDGFRalpha (unknown origin) using myelin basic protein as substrat... 38850857
Macrophage colony-stimulating factor 1 receptor IC50 = 1347.0 nM 5.87 Inhibition of NanoLuc-fused FMS (unknown origin) transfected in HEK293 cells by ... 38850857
Hep 3B2 IC50 = 1790.0 nM 5.75 Antiproliferative activity against human Hep3B cells assessed as cell growth inh... 38850857
HepG2 IC50 = 2370.0 nM 5.62 Antiproliferative activity against human HepG2 cells assessed as cell growth inh... 38850857
HS27 IC50 = 8800.0 nM 5.06 Cytotoxicity against human HS27 cells assessed as reduction in cell growth measu... 38850857
WI-38 IC50 = 16700.0 nM 4.78 Cytotoxicity against human WI-38 cells assessed as reduction in cell growth meas... 38850857
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 83450.0 nM 4.08 Inhibition of fluorescence tracer red binding to human ERG measured after 3 hrs ... 38850857

Literature References

Data from ChEMBL 36 via Core Engine