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Compound Detail

CHEMBL1614773

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C[C@@H]1COCCN1c1cc(-c2ccc3c(N)[nH]nc3c2)nc(N)n1

Basic Information

ChEMBL ID CHEMBL1614773
Phase Preclinical
Structure Type MOL
InChI Key WNVXQKKSIHKYCX-SECBINFHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

325.4
MW (Da)
1.41
ALogP
7
HBA
3
HBD
119.0
PSA (Ų)
0.65
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19N7O
MW 325.38
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.14

Activity Summary

IC50 4 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
IC50 7.2 7.2 63.1 1
Aurora kinase A
CHEMBL4722
IC50 4.9 4.9 12589.2 1
Rho-associated protein kinase 1
CHEMBL3231
IC50 4.8 4.8 15848.9 1
Aurora kinase B
CHEMBL2185
IC50 4.6 4.6 25118.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3-phosphoinositide-dependent protein kinase 1 IC50 = 63.1 nM 7.2 Inhibition of PDK1 21341675
Aurora kinase A IC50 = 12589.25 nM 4.9 Inhibition of aurora A 21341675
Rho-associated protein kinase 1 IC50 = 15848.93 nM 4.8 Inhibition of ROCK1 21341675
Aurora kinase B IC50 = 25118.86 nM 4.6 Inhibition of aurora B 21341675

Literature References

PubMed DOI Target Context # Activities
21341675 10.1021/jm101527u 3-phosphoinositide-dependent protein kinase 1 1
21341675 10.1021/jm101527u Aurora kinase A 1
21341675 10.1021/jm101527u Aurora kinase B 1
21341675 10.1021/jm101527u TGF-beta receptor type-1 1
21341675 10.1021/jm101527u Rho-associated protein kinase 1 1

Data from ChEMBL 36 via Core Engine