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Compound Detail

CHEMBL5598003

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CNC(=O)c1cc(-c2ccc(NC(=O)Nc3ccc(N4CCN(C)CC4)c(C(F)(F)F)c3)cc2)nc2cccnc12

Basic Information

ChEMBL ID CHEMBL5598003
Phase Preclinical
Structure Type MOL
InChI Key ZUBOCRXKKDKIIK-UHFFFAOYSA-N
10
Targets
12
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

563.6
MW (Da)
5.07
ALogP
6
HBA
3
HBD
102.5
PSA (Ų)
0.31
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28F3N7O2
MW 563.58
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.57

Activity Summary

IC50 12 meas. best 7.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 7.67 7.1967 21.4 3
BMDM
CHEMBL4296525
IC50 7.25 7.25 56.0 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
IC50 6.44 6.44 366.3 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.44 6.44 362.0 1
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 6.01 6.01 972.4 1
HepG2
CHEMBL395
IC50 5.83 5.83 1480.0 1
Hep 3B2
CHEMBL4296437
IC50 5.79 5.79 1630.0 1
HS27
CHEMBL614666
IC50 5.03 5.03 9400.0 1
WI-38
CHEMBL614391
IC50 4.72 4.72 19100.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.02 4.02 95900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Macrophage colony-stimulating factor 1 receptor IC50 = 21.5 nM 7.67 Inhibition of FMS (unknown origin) using myelin basic protein as substrate measu... 38850857
Macrophage colony-stimulating factor 1 receptor IC50 = 21.38 nM 7.67 Inhibition of FMS (unknown origin) using myelin basic protein as substrate measu... 38850857
BMDM IC50 = 56.0 nM 7.25 Inhibition of CSF-1-induced C57BL6 mouse BMDM cell growth preincubated for 1 hr ... 38850857
Receptor-type tyrosine-protein kinase FLT3 IC50 = 362.0 nM 6.44 Inhibition of FLT3 (unknown origin) using myelin basic protein as substrate meas... 38850857
Vascular endothelial growth factor receptor 3 IC50 = 366.3 nM 6.44 Inhibition of FLT4 (unknown origin) using myelin basic protein as substrate meas... 38850857
Macrophage colony-stimulating factor 1 receptor IC50 = 563.0 nM 6.25 Inhibition of NanoLuc-fused FMS (unknown origin) transfected in HEK293 cells by ... 38850857
Platelet-derived growth factor receptor alpha IC50 = 972.4 nM 6.01 Inhibition of PDGFRalpha (unknown origin) using myelin basic protein as substrat... 38850857
HepG2 IC50 = 1480.0 nM 5.83 Antiproliferative activity against human HepG2 cells assessed as cell growth inh... 38850857
Hep 3B2 IC50 = 1630.0 nM 5.79 Antiproliferative activity against human Hep3B cells assessed as cell growth inh... 38850857
HS27 IC50 = 9400.0 nM 5.03 Cytotoxicity against human HS27 cells assessed as reduction in cell growth measu... 38850857
WI-38 IC50 = 19100.0 nM 4.72 Cytotoxicity against human WI-38 cells assessed as reduction in cell growth meas... 38850857
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 95900.0 nM 4.02 Inhibition of fluorescence tracer red binding to human ERG measured after 3 hrs ... 38850857

Literature References

PubMed DOI Target Context # Activities
38850857 10.1016/j.ejmech.2024.116557 Hep 3B2 9
38850857 10.1016/j.ejmech.2024.116557 Macrophage colony-stimulating factor 1 receptor 6
38850857 10.1016/j.ejmech.2024.116557 HepG2 3
38850857 10.1016/j.ejmech.2024.116557 NT-3 growth factor receptor 2
38850857 10.1016/j.ejmech.2024.116557 Voltage-gated inwardly rectifying potassium channel KCNH2 2
38850857 10.1016/j.ejmech.2024.116557 Platelet-derived growth factor receptor alpha 2
38850857 10.1016/j.ejmech.2024.116557 High affinity nerve growth factor receptor 2
38850857 10.1016/j.ejmech.2024.116557 Receptor-type tyrosine-protein kinase FLT3 2
38850857 10.1016/j.ejmech.2024.116557 Vascular endothelial growth factor receptor 3 2
38850857 10.1016/j.ejmech.2024.116557 BMDM 2
38850857 10.1016/j.ejmech.2024.116557 HT-29 1
38850857 10.1016/j.ejmech.2024.116557 M14 1
38850857 10.1016/j.ejmech.2024.116557 SF-539 1
38850857 10.1016/j.ejmech.2024.116557 SF-295 1
38850857 10.1016/j.ejmech.2024.116557 SW-620 1
38850857 10.1016/j.ejmech.2024.116557 HCT-116 1
38850857 10.1016/j.ejmech.2024.116557 COLO 205 1
38850857 10.1016/j.ejmech.2024.116557 A549 1
38850857 10.1016/j.ejmech.2024.116557 SR 1
38850857 10.1016/j.ejmech.2024.116557 K562 1

Data from ChEMBL 36 via Core Engine