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Compound Detail

CHEMBL3290631

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CC1=CC(=O)N(Nc2nc(-c3cccs3)nc3scc(-c4cccc(OCCN5CCCCC5)c4)c23)C1=O.Cl

Basic Information

ChEMBL ID CHEMBL3290631
Phase Preclinical
Structure Type MOL
InChI Key SBXOZKDGWVQQCI-UHFFFAOYSA-N
Parent Compound CHEMBL3305003
Active Moiety CHEMBL3305003
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

545.7
MW (Da)
5.59
ALogP
9
HBA
1
HBD
87.7
PSA (Ų)
0.29
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H28ClN5O3S2
MW 582.15
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.50

Activity Summary

IC50 3 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.88 6.88 133.0 1
RAW264.7
CHEMBL612557
IC50 5.67 5.605 2150.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24813730 10.1016/j.bmcl.2014.04.058 Inhibitor of nuclear factor kappa-B kinase subunit beta 3
24813730 10.1016/j.bmcl.2014.04.058 RAW264.7 2
24813730 10.1016/j.bmcl.2014.04.058 Receptor-type tyrosine-protein kinase FLT3 2
24813730 10.1016/j.bmcl.2014.04.058 Mitogen-activated protein kinase 12 1
24813730 10.1016/j.bmcl.2014.04.058 Tyrosine-protein kinase Lck 1
24813730 10.1016/j.bmcl.2014.04.058 Mitogen-activated protein kinase 8 1
24813730 10.1016/j.bmcl.2014.04.058 Tyrosine-protein kinase JAK1 1
24813730 10.1016/j.bmcl.2014.04.058 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
24813730 10.1016/j.bmcl.2014.04.058 Tyrosine-protein kinase BTK 1
24813730 10.1016/j.bmcl.2014.04.058 Non-receptor tyrosine-protein kinase TYK2 1
24813730 10.1016/j.bmcl.2014.04.058 Mitogen-activated protein kinase 13 1
24813730 10.1016/j.bmcl.2014.04.058 Tyrosine-protein kinase Lyn 1
24813730 10.1016/j.bmcl.2014.04.058 Mitogen-activated protein kinase 11 1
24813730 10.1016/j.bmcl.2014.04.058 Mitogen-activated protein kinase 14 1
24813730 10.1016/j.bmcl.2014.04.058 Rho-associated protein kinase 2 1
24813730 10.1016/j.bmcl.2014.04.058 Unchecked 1
24813730 10.1016/j.bmcl.2014.04.058 Ribosomal protein S6 kinase alpha-5 1
24813730 10.1016/j.bmcl.2014.04.058 Dual specificity mitogen-activated protein kinase kinase 7 1
24813730 10.1016/j.bmcl.2014.04.058 Dual specificity mitogen-activated protein kinase kinase 6 1
24813730 10.1016/j.bmcl.2014.04.058 Dual specificity mitogen-activated protein kinase kinase 4 1

Data from ChEMBL 36 via Core Engine