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Compound Detail

CHEMBL1765731

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Nc1nc(-c2ccc3c(N)n[nH]c3c2)cc(N2CCO[C@@H](C(=O)Nc3ccccc3)C2)n1

Basic Information

ChEMBL ID CHEMBL1765731
Phase Preclinical
Structure Type MOL
InChI Key NCSQDKMOKNQGSG-GOSISDBHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
2.03
ALogP
8
HBA
4
HBD
148.1
PSA (Ų)
0.38
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N8O2
MW 430.47
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.46

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3-phosphoinositide-dependent protein kinase 1 IC50 = 1000.0 nM 6.0 Inhibition of PDK1 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