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Compound Detail

CHEMBL56904

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CN1CCN(Cc2ccc(C(=O)Nc3cccc(Nc4nccc(-c5cccnc5)n4)c3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL56904
Phase Preclinical
Structure Type MOL
InChI Key JHMBUEWQJDGKGS-UHFFFAOYSA-N
7
Targets
9
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

479.6
MW (Da)
4.28
ALogP
7
HBA
2
HBD
86.3
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C28H29N7O
MW 479.59
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.72

Activity Summary

IC50 8 meas. best 7.0
Ki 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 7.0 7.0 100.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 7.0 7.0 100.0 1
BCR/ABL1
CHEMBL4523652
IC50 7.0 7.0 100.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 6.8 6.8 160.0 1
Platelet-derived growth factor receptor
CHEMBL2095189
IC50 6.7 6.7 200.0 1
Platelet-derived growth factor receptor beta
CHEMBL2749
IC50 6.7 6.7 200.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 5.11 5.11 7800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 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
- 10.1016/S0960-894X(96)00601-4 No relevant target 1
22257213 10.1021/jm201271b Tyrosine-protein kinase SYK 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1
30243589 10.1016/j.bmcl.2018.09.016 BCR/ABL1 1
30243589 10.1016/j.bmcl.2018.09.016 Platelet-derived growth factor receptor beta 1
30243589 10.1016/j.bmcl.2018.09.016 Proto-oncogene tyrosine-protein kinase Src 1
30243589 10.1016/j.bmcl.2018.09.016 cAMP-dependent protein kinase (PKA) 1
30243589 10.1016/j.bmcl.2018.09.016 Protein kinase C (PKC) 1

Data from ChEMBL 36 via Core Engine