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Compound Detail

CHEMBL440847

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COc1cc2c(Nc3cc(OC)c(OC)c(OC)c3)c(C#N)cnc2cc1OCC1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL440847
Phase Preclinical
Structure Type MOL
InChI Key BWLSIYJKVFXNFV-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

492.6
MW (Da)
4.61
ALogP
9
HBA
1
HBD
98.1
PSA (Ų)
0.46
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N4O5
MW 492.58
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.85

Activity Summary

IC50 7 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 8.08 7.77 8.3 2
Tyrosine-protein kinase ABL
CHEMBL2111414
IC50 7.92 7.92 12.0 1
KU812 cell line
CHEMBL613997
IC50 7.16 7.16 70.0 1
K562
CHEMBL385
IC50 6.85 6.85 140.0 1
Src-transformed
CHEMBL614302
IC50 5.8 5.8 1600.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14552782 10.1016/j.bmcl.2003.07.001 Proto-oncogene tyrosine-protein kinase Src 1
14552782 10.1016/j.bmcl.2003.07.001 Src-transformed 1
15027848 10.1021/jm0499458 Proto-oncogene tyrosine-protein kinase Src 1
15027848 10.1021/jm0499458 Src-transformed 1
15027848 10.1021/jm0499458 Tyrosine-protein kinase ABL 1
15027848 10.1021/jm0499458 KU812 cell line 1
15027848 10.1021/jm0499458 K562 1

Data from ChEMBL 36 via Core Engine