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Compound Detail

CHEMBL225224

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O=C(NCc1c(Cl)cccc1Cl)Nc1ccc2[nH]ncc2c1

Basic Information

ChEMBL ID CHEMBL225224
Phase Preclinical
Structure Type MOL
InChI Key HCDNKTJUMCHZJG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

335.2
MW (Da)
4.19
ALogP
2
HBA
3
HBD
69.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12Cl2N4O
MW 335.19
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -2.19

Activity Summary

IC50 3 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase
CHEMBL2111459
IC50 7.7 7.7 20.0 1
Rho-associated protein kinase 2
CHEMBL2973
IC50 7.7 7.7 20.0 1
Unchecked
CHEMBL612545
IC50 7.7 7.7 19.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase IC50 = 20.0 nM 7.7 Inhibition of Rho kinase 17046269
Unchecked IC50 = 19.95 nM 7.7 Inhibition of ROCK 20347188
Rho-associated protein kinase 2 IC50 = 20.0 nM 7.7 Inhibition of ROCK2 (unknown origin) 26486225

Literature References

PubMed DOI Target Context # Activities
17046269 10.1016/j.bmc.2006.09.052 Rho-associated protein kinase 1
17046269 10.1016/j.bmc.2006.09.052 C-C chemokine receptor type 2 1
20347188 10.1016/j.ejmech.2010.02.059 Unchecked 1
26486225 10.1021/acs.jmedchem.5b00683 Rho-associated protein kinase 2 1

Data from ChEMBL 36 via Core Engine