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Compound Detail

CHEMBL2059162

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

Basic Information

ChEMBL ID CHEMBL2059162
Phase Preclinical
Structure Type MOL
InChI Key VCEUQTKYYDRYLK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
2.65
ALogP
4
HBA
4
HBD
112.9
PSA (Ų)
0.39
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21N5O2
MW 351.41
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calmodulin-domain protein kinase 1
CHEMBL1781862
IC50 6.85 6.85 140.0 1
Unchecked
CHEMBL612545
IC50 6.82 6.82 150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calmodulin-domain protein kinase 1 IC50 = 140.0 nM 6.85 Inhibition of Toxoplasma gondii CDPK1 22795629
Unchecked IC50 = 150.0 nM 6.82 Inhibition of Cryptosporidium parvum CDPK1 22795629

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 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