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Compound Detail

CHEMBL370773

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COc1cc(-c2nn(C3CCN(C4CCN(C(C)=O)CC4)CC3)c3ncnc(N)c23)ccc1NC(=O)c1cc2ccccc2n1C

Basic Information

ChEMBL ID CHEMBL370773
Phase Preclinical
Structure Type MOL
InChI Key QFNDMWXKSLDXLR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

621.8
MW (Da)
4.48
ALogP
10
HBA
2
HBD
136.4
PSA (Ų)
0.28
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H39N9O3
MW 621.75
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.27

Activity Summary

IC50 2 meas. best 7.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.13 7.13 74.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 4.77 4.77 17150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase Lck IC50 = 74.0 nM 7.13 Inhibitory activity against lck 16216497
Proto-oncogene tyrosine-protein kinase Src IC50 = 17150.0 nM 4.77 Inhibitory activity against src 16216497

Literature References

PubMed DOI Target Context # Activities
16216497 10.1016/j.bmcl.2005.09.039 Proto-oncogene tyrosine-protein kinase LCK 2
16216497 10.1016/j.bmcl.2005.09.039 Tyrosine-protein kinase Lck 1
16216497 10.1016/j.bmcl.2005.09.039 Proto-oncogene tyrosine-protein kinase Src 1
16216497 10.1016/j.bmcl.2005.09.039 Tyrosine-protein kinase Fyn 1

Data from ChEMBL 36 via Core Engine