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Compound Detail

CHEMBL498070

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N#Cc1cnc2c(Cl)cc(NCc3cn(Cc4ccncc4)nn3)cc2c1Nc1ccc(F)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL498070
Phase Preclinical
Structure Type MOL
InChI Key MSCFFMOQZYEWFY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

519.4
MW (Da)
5.94
ALogP
8
HBA
2
HBD
104.3
PSA (Ų)
0.27
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 C25H17Cl2FN8
MW 519.37
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -2.15

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 8.4 8.4 4.0 1
Blood
CHEMBL613416
IC50 5.55 5.55 2800.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 88.0 mL.min-1.kg-1 Rattus norvegicus

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 Rattus norvegicus 1
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

Data from ChEMBL 36 via Core Engine