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Compound Detail

CHEMBL5278924

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O=C(CCCC1CCSS1)N1CCCN(S(=O)(=O)c2cccc3cnccc23)CC1

Basic Information

ChEMBL ID CHEMBL5278924
Phase Preclinical
Structure Type MOL
InChI Key RWRIQCPRDVTYTG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

465.7
MW (Da)
3.78
ALogP
6
HBA
0
HBD
70.6
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27N3O3S3
MW 465.67
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.35

Activity Summary

IC50 2 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 1
CHEMBL3231
IC50 5.8 5.8 1590.0 1
Rho-associated protein kinase 2
CHEMBL2973
IC50 5.68 5.68 2100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase 1 IC50 = 1590.0 nM 5.8 Inhibition of ROCK1 (unknown origin) 34388381
Rho-associated protein kinase 2 IC50 = 2100.0 nM 5.68 Inhibition of ROCK2 (unknown origin) 34388381

Literature References

PubMed DOI Target Context # Activities
34388381 10.1016/j.ejmech.2021.113742 Rho-associated protein kinase 1 1
34388381 10.1016/j.ejmech.2021.113742 Rho-associated protein kinase 2 1

Data from ChEMBL 36 via Core Engine