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Compound Detail

CHEMBL227727

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NCCc1ccc(-c2ncnc3[nH]cnc23)cc1

Basic Information

ChEMBL ID CHEMBL227727
Phase Preclinical
Structure Type MOL
InChI Key AOXVRIHLGDJGQV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

239.3
MW (Da)
1.52
ALogP
4
HBA
2
HBD
80.5
PSA (Ų)
0.73
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H13N5
MW 239.28
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -0.26

Activity Summary

IC50 1 meas. best 5.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 5.02 5.02 9500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-beta serine/threonine-protein kinase IC50 = 9500.0 nM 5.02 Inhibition of PKBbeta by radiometric filter binding assay 17451235

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C3MD00308F Tyrosine-protein kinase ABL1 4
- 10.1039/C3MD00308F cGMP-dependent protein kinase 1 2
- 10.1039/C3MD00308F Unchecked 2
- 10.1039/C3MD00308F Protein kinase C beta type 2
- 10.1039/C3MD00308F Receptor-type tyrosine-protein kinase FLT3 2
- 10.1039/C3MD00308F Fibroblast growth factor receptor 2 2
- 10.1039/C3MD00308F Mitogen-activated protein kinase 12 1
- 10.1039/C3MD00308F Serine/threonine-protein kinase D2 1
- 10.1039/C3MD00308F Serine/threonine-protein kinase Chk2 1
- 10.1039/C3MD00308F Mitogen-activated protein kinase 1 1
- 10.1039/C3MD00308F Mitogen-activated protein kinase 3 1
- 10.1039/C3MD00308F Mitogen-activated protein kinase 14 1
- 10.1039/C3MD00308F MAP kinase p38 1
- 10.1039/C3MD00308F Mitogen-activated protein kinase 13 1
- 10.1039/C3MD00308F Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
- 10.1039/C3MD00308F Aurora kinase A 1
- 10.1039/C3MD00308F Aurora kinase C 1
- 10.1039/C3MD00308F Inhibitor of nuclear factor kappa-B kinase subunit beta 1
- 10.1039/C3MD00308F Serine/threonine-protein kinase Nek2 1
17451235 10.1021/jm0700924 PC-3M 1

Data from ChEMBL 36 via Core Engine