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Compound Detail

CHEMBL493875

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CCn1c(-c2nonc2N)nc2c(C#CCCO)ncc(OCCCN)c21

Basic Information

ChEMBL ID CHEMBL493875
Phase Preclinical
Structure Type MOL
InChI Key BNYVNKCEEQZWJL-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

371.4
MW (Da)
0.54
ALogP
10
HBA
3
HBD
151.1
PSA (Ų)
0.40
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21N7O3
MW 371.40
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.65

Activity Summary

IC50 4 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ribosomal protein S6 kinase alpha-1
CHEMBL2553
IC50 8.22 8.22 6.0 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 7.3 6.255 50.0 2
Rho-associated protein kinase 1
CHEMBL3231
IC50 6.9 6.9 126.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18800763 10.1021/jm8004527 RAC-alpha serine/threonine-protein kinase 2
18800763 10.1021/jm8004527 Ribosomal protein S6 kinase alpha-5 1
18800763 10.1021/jm8004527 Rho-associated protein kinase 1 1
18800763 10.1021/jm8004527 Ribosomal protein S6 kinase alpha-1 1

Data from ChEMBL 36 via Core Engine