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Compound Detail

CHEMBL423288

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CC(=O)Nc1ccc(C)c(Nc2nccc(-c3cccnc3)n2)c1

Basic Information

ChEMBL ID CHEMBL423288
Phase Preclinical
Structure Type MOL
InChI Key PMGVYOWQUQXHSP-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
3.55
ALogP
5
HBA
2
HBD
79.8
PSA (Ų)
0.77
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17N5O
MW 319.37
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.83

Activity Summary

IC50 6 meas. best 5.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 5.24 5.24 5800.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 5.24 5.24 5754.4 1
Platelet-derived growth factor receptor
CHEMBL2095189
IC50 4.3 4.3 50000.0 2
Platelet-derived growth factor receptor
CHEMBL2096980
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00197-7 Platelet-derived growth factor receptor 1
- 10.1016/0960-894X(96)00197-7 Epidermal growth factor receptor 1
- 10.1016/0960-894X(96)00197-7 Proto-oncogene tyrosine-protein kinase Src 1
- 10.1016/0960-894X(96)00197-7 Protein kinase C alpha type 1
- 10.1016/0960-894X(96)00197-7 Protein kinase C delta type 1
- 10.1016/0960-894X(96)00197-7 cAMP-dependent protein kinase (PKA) 1
- 10.1016/S0960-894X(96)00601-4 Tyrosine-protein kinase ABL1 1
- 10.1016/S0960-894X(96)00601-4 Epidermal growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 Proto-oncogene tyrosine-protein kinase Src 1
- 10.1016/S0960-894X(96)00601-4 Platelet-derived growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 cAMP-dependent protein kinase (PKA) 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C alpha type 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C delta type 1
17983688 10.1016/j.ejmech.2007.09.021 Platelet-derived growth factor receptor 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1
30873837 10.1021/acs.jmedchem.8b02007 Unchecked 1

Data from ChEMBL 36 via Core Engine