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Compound Detail

CHEMBL20867

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Cc1ccc(C(=O)Nc2ccc(C)c(Nc3nccc(-c4cccnc4)n3)c2)cc1

Basic Information

ChEMBL ID CHEMBL20867
Phase Preclinical
Structure Type MOL
InChI Key SZJRFGYYRZITCZ-UHFFFAOYSA-N
3
Targets
7
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

395.5
MW (Da)
5.15
ALogP
5
HBA
2
HBD
79.8
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21N5O
MW 395.47
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.78

Activity Summary

IC50 7 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor
CHEMBL2095189
IC50 8.0 8.0 10.0 3
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 7.7 7.2 20.0 2
Bcr/Abl fusion protein
CHEMBL2096618
IC50 6.7 6.7 199.5 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(96)00601-4 cAMP-dependent protein kinase (PKA) 1
29945794 10.1016/j.bmcl.2018.06.043 Bcr/Abl fusion protein 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1
16220969 10.1021/jm058225d Proto-oncogene tyrosine-protein kinase Src 1
16220969 10.1021/jm058225d Tyrosine-protein kinase ABL1 1
16220969 10.1021/jm058225d Protein kinase C alpha type 1
16220969 10.1021/jm058225d Platelet-derived growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 No relevant target 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C delta type 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C alpha type 1
- 10.1016/0960-894X(96)00197-7 Platelet-derived growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 Platelet-derived 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 Epidermal growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 Tyrosine-protein kinase ABL1 1
- 10.1016/0960-894X(96)00197-7 cAMP-dependent protein kinase (PKA) 1
- 10.1016/0960-894X(96)00197-7 Protein kinase C delta type 1
- 10.1016/0960-894X(96)00197-7 Protein kinase C alpha type 1
- 10.1016/0960-894X(96)00197-7 Proto-oncogene tyrosine-protein kinase Src 1
- 10.1016/0960-894X(96)00197-7 Epidermal growth factor receptor 1

Data from ChEMBL 36 via Core Engine