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Compound Detail

CHEMBL1765748

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CC(C)(C)OC(=O)N[C@@H]1CCCN(c2cc(-c3ccc4c(N)n[nH]c4c3)nc(N)n2)C1

Basic Information

ChEMBL ID CHEMBL1765748
Phase Preclinical
Structure Type MOL
InChI Key HVNQYDHDQBJAAH-CYBMUJFWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

424.5
MW (Da)
2.68
ALogP
8
HBA
4
HBD
148.1
PSA (Ų)
0.50
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 C21H28N8O2
MW 424.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.39

Activity Summary

IC50 3 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
IC50 7.6 7.6 25.1 1
Aurora kinase A
CHEMBL4722
IC50 5.8 5.8 1584.9 1
Aurora kinase B
CHEMBL2185
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 = 25.12 nM 7.6 Inhibition of PDK1 21341675
Aurora kinase A IC50 = 1584.89 nM 5.8 Inhibition of aurora A 21341675
Aurora kinase B IC50 = 5011.87 nM 5.3 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