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Compound Detail

CHEMBL1765757

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CC(C)c1cc(-c2ccc3c(N)n[nH]c3c2)nc(N)n1

Basic Information

ChEMBL ID CHEMBL1765757
Phase Preclinical
Structure Type MOL
InChI Key VBJULRMRDQBSIN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

268.3
MW (Da)
2.31
ALogP
5
HBA
3
HBD
106.5
PSA (Ų)
0.66
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 C14H16N6
MW 268.32
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.79

Activity Summary

IC50 4 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
IC50 6.6 6.6 251.2 1
TGF-beta receptor type-1
CHEMBL4439
IC50 5.7 5.7 1995.3 1
Aurora kinase A
CHEMBL4722
IC50 5.5 5.5 3162.3 1
Aurora kinase B
CHEMBL2185
IC50 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3-phosphoinositide-dependent protein kinase 1 IC50 = 251.19 nM 6.6 Inhibition of PDK1 21341675
TGF-beta receptor type-1 IC50 = 1995.26 nM 5.7 Inhibition of ALK5 21341675
Aurora kinase A IC50 = 3162.28 nM 5.5 Inhibition of aurora A 21341675
Aurora kinase B IC50 = 7943.28 nM 5.1 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
- 10.6019/CHEMBL3988181 Unchecked 1

Data from ChEMBL 36 via Core Engine