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Compound Detail

CHEMBL2059165

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O=C(NCCC1CCCNC1)Nc1nc2ccc(C(=O)c3ccccc3)cc2[nH]1

Basic Information

ChEMBL ID CHEMBL2059165
Phase Preclinical
Structure Type MOL
InChI Key GKDGNKRGOJPYMM-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

391.5
MW (Da)
3.31
ALogP
4
HBA
4
HBD
98.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N5O2
MW 391.48
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.05

Activity Summary

IC50 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 8.0 8.0 10.0 2
Calmodulin-domain protein kinase 1
CHEMBL1781862
IC50 6.92 6.92 120.0 1
Unchecked
CHEMBL612545
IC50 6.8 6.8 160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22795629 10.1016/j.bmcl.2012.06.050 Calmodulin-domain protein kinase 1 1
22795629 10.1016/j.bmcl.2012.06.050 Unchecked 1
22795629 10.1016/j.bmcl.2012.06.050 Tyrosine-protein kinase ABL1 1
22795629 10.1016/j.bmcl.2012.06.050 Toxoplasma gondii 1
22795629 10.1016/j.bmcl.2012.06.050 Cryptosporidium parvum 1
22795629 10.1016/j.bmcl.2012.06.050 HL-60 1
22795629 10.1016/j.bmcl.2012.06.050 ADMET 1

Data from ChEMBL 36 via Core Engine