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Compound Detail

CHEMBL498028

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N#Cc1cnc2c(Cl)cc(NCc3cn(C4CCNCC4)nn3)cc2c1Nc1ccc(F)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL498028
Phase Preclinical
Structure Type MOL
InChI Key YIFLRNURKJVDHB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

511.4
MW (Da)
5.42
ALogP
8
HBA
3
HBD
103.5
PSA (Ų)
0.32
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21Cl2FN8
MW 511.39
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.95

Activity Summary

IC50 2 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 8.28 8.28 5.3 1
Blood
CHEMBL613416
IC50 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19464884 10.1016/j.bmcl.2009.05.009 Unchecked 6
19464884 10.1016/j.bmcl.2009.05.009 No relevant target 2
19464884 10.1016/j.bmcl.2009.05.009 Mitogen-activated protein kinase kinase kinase 8 1
19464884 10.1016/j.bmcl.2009.05.009 Blood 1
19464884 10.1016/j.bmcl.2009.05.009 ADMET 1

Data from ChEMBL 36 via Core Engine