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Compound Detail

CHEMBL1765728

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CC[C@@H]1COCCN1c1cc(-c2ccc3c(N)n[nH]c3c2)nc(N)n1

Basic Information

ChEMBL ID CHEMBL1765728
Phase Preclinical
Structure Type MOL
InChI Key NOAWVMJDSNKUAH-LLVKDONJSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

339.4
MW (Da)
1.80
ALogP
7
HBA
3
HBD
119.0
PSA (Ų)
0.67
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21N7O
MW 339.40
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.02

Activity Summary

IC50 2 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
IC50 7.5 7.5 31.6 1
Aurora kinase A
CHEMBL4722
IC50 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3-phosphoinositide-dependent protein kinase 1 IC50 = 31.62 nM 7.5 Inhibition of PDK1 21341675
Aurora kinase A IC50 = 5011.87 nM 5.3 Inhibition of aurora A 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