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Compound Detail

CHEMBL524638

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N#Cc1cnc2c(Br)cc(NCc3cn(Cc4cccnc4)nn3)cc2c1Nc1ccc(F)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL524638
Phase Preclinical
Structure Type MOL
InChI Key NDZILMRCELWAKE-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

563.8
MW (Da)
6.05
ALogP
8
HBA
2
HBD
104.3
PSA (Ų)
0.25
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 C25H17BrClFN8
MW 563.82
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -2.27

Activity Summary

IC50 3 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 7.7 7.7 20.0 1
Monocyte
CHEMBL614076
IC50 6.66 6.66 220.0 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 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
19464884 10.1016/j.bmcl.2009.05.009 Monocyte 1
19464884 10.1016/j.bmcl.2009.05.009 ADMET 1

Data from ChEMBL 36 via Core Engine