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Compound Detail

CHEMBL5175332

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CC(C)NC[C@@H](C(=O)N1CCN(c2ncnc3c2[C@H](C)OC(=O)N3)CC1)c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL5175332
Phase Preclinical
Structure Type MOL
InChI Key DHMFFVNUPLZBKN-MAUKXSAKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

473.0
MW (Da)
3.18
ALogP
7
HBA
2
HBD
99.7
PSA (Ų)
0.67
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29ClN6O3
MW 472.98
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.80

Activity Summary

IC50 3 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
IC50 9.7 9.7 0.2 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 8.82 8.82 1.5 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35679512 10.1021/acs.jmedchem.2c00527 RAC-alpha serine/threonine-protein kinase 1
35679512 10.1021/acs.jmedchem.2c00527 RAC-beta serine/threonine-protein kinase 1
35679512 10.1021/acs.jmedchem.2c00527 RAC-gamma serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine