Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL2023714

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
N=C(N)NCCC[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)CCCCCNCCNS(=O)(=O)c1cccc2cnccc12)C(N)=O

Basic Information

ChEMBL ID CHEMBL2023714
Phase Preclinical
Structure Type MOL
InChI Key DWZCDSLYZDTWQH-JCUPRAGWSA-N
6
Targets
14
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

1301.6
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C53H96N28O9S
MW 1301.60

Activity Summary

IC50 9 meas. best 8.61
Kd 5 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 9.28 7.645 0.5 2
Rho-associated protein kinase 2
CHEMBL2973
IC50 8.61 8.61 2.5 2
Unchecked
CHEMBL612545
IC50 8.26 7.4267 5.5 3
Ribosomal protein S6 kinase beta-1
CHEMBL4501
IC50 8.19 8.19 6.5 1
cGMP-dependent protein kinase 1
CHEMBL4273
Kd 7.89 7.89 13.0 1
Ribosomal protein S6 kinase alpha-5
CHEMBL4237
Kd 7.58 7.58 26.0 1
cGMP-dependent protein kinase 1
CHEMBL4273
IC50 7.38 7.38 41.7 1
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
Kd 7.26 7.26 55.0 1
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
IC50 7.14 7.14 72.4 1
Ribosomal protein S6 kinase alpha-5
CHEMBL4237
IC50 7.09 7.09 81.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Kd = 0.53 nM 9.28 Displacement of fluorescent-ARC-583 from recombinant bovine PKAc by fluorescence... 22521647
Rho-associated protein kinase 2 IC50 = 2.455 nM 8.61 Displacement of fluorescent-ARC-1042 from His6-tagged recombinant human ROCK2 by... 22521647
Rho-associated protein kinase 2 IC50 = 2.455 nM 8.61 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
Unchecked IC50 = 5.495 nM 8.26 Displacement of fluorescent-ARC-583 from recombinant bovine PKAc by fluorescence... 22521647
Unchecked IC50 = 5.495 nM 8.26 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from recombinant bovine PK... 22521647
Ribosomal protein S6 kinase beta-1 IC50 = 6.457 nM 8.19 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
cGMP-dependent protein kinase 1 Kd = 13.0 nM 7.89 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
Ribosomal protein S6 kinase alpha-5 Kd = 26.0 nM 7.58 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
cGMP-dependent protein kinase 1 IC50 = 41.69 nM 7.38 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
RAC-gamma serine/threonine-protein kinase Kd = 55.0 nM 7.26 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
RAC-gamma serine/threonine-protein kinase IC50 = 72.44 nM 7.14 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
Ribosomal protein S6 kinase alpha-5 IC50 = 81.28 nM 7.09 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
Unchecked Kd = 980.0 nM 6.01 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647
Unchecked IC50 = 1737.8 nM 5.76 Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombina... 22521647

Literature References

PubMed DOI Target Context # Activities
22521647 10.1016/j.bmcl.2012.03.101 Unchecked 6
22521647 10.1016/j.bmcl.2012.03.101 Rho-associated protein kinase 2 4
22521647 10.1016/j.bmcl.2012.03.101 RAC-gamma serine/threonine-protein kinase 2
22521647 10.1016/j.bmcl.2012.03.101 Ribosomal protein S6 kinase alpha-5 2
22521647 10.1016/j.bmcl.2012.03.101 Ribosomal protein S6 kinase beta-1 2
22521647 10.1016/j.bmcl.2012.03.101 cGMP-dependent protein kinase 1 2

Data from ChEMBL 36 via Core Engine