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Compound Detail

CHEMBL425834

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CN(C)CCCn1cc(CNc2cc(Br)c3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)nn1

Basic Information

ChEMBL ID CHEMBL425834
Phase Preclinical
Structure Type MOL
InChI Key RUCXDAGQSXXFMK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
14
Publications
0
Known Names

Molecular Properties

557.9
MW (Da)
5.56
ALogP
8
HBA
2
HBD
94.7
PSA (Ų)
0.28
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23BrClFN8
MW 557.86
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -2.26

Activity Summary

IC50 2 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
CaM kinase II
CHEMBL2097164
IC50 5.25 5.25 5600.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Rattus norvegicus
F - % Rattus norvegicus
t1/2 - - Rattus norvegicus
T1/2 2.6 hr Rattus norvegicus
Vss - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase kinase kinase 8 IC50 = 20.0 nM 7.7 Inhibition of Tpl2 by ELISA 17715908
CaM kinase II IC50 = 5600.0 nM 5.25 Inhibition of CAMK2 17715908

Literature References

PubMed DOI Target Context # Activities
17715908 10.1021/jm070436q Rattus norvegicus 6
17715908 10.1021/jm070436q Mitogen-activated protein kinase kinase kinase 8 1
17715908 10.1021/jm070436q Epidermal growth factor receptor 1
17715908 10.1021/jm070436q Monocyte 1
17715908 10.1021/jm070436q Blood 1
17715908 10.1021/jm070436q Mitogen-activated protein kinase 14 1
17715908 10.1021/jm070436q CaM kinase II 1
17715908 10.1021/jm070436q Protein kinase C alpha type 1
17715908 10.1021/jm070436q cAMP-dependent protein kinase (PKA) 1
17715908 10.1021/jm070436q MAP kinase-activated protein kinase 2 1
17715908 10.1021/jm070436q Proto-oncogene tyrosine-protein kinase Src 1
17715908 10.1021/jm070436q Ribosomal protein S6 kinase beta-1 1
17715908 10.1021/jm070436q Mitogen-activated protein kinase 8 1
17715908 10.1021/jm070436q Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine