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Compound Detail

CHEMBL224887

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O=C(NCc1ccc(Cl)cc1Cl)Nc1ccc2[nH]ncc2c1

Basic Information

ChEMBL ID CHEMBL224887
Phase Preclinical
Structure Type MOL
InChI Key QFYWQJFCTRAAGF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
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 -2.48

Activity Summary

IC50 2 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase
CHEMBL2111459
IC50 6.66 6.66 220.0 1
Unchecked
CHEMBL612545
IC50 6.66 6.66 218.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase IC50 = 220.0 nM 6.66 Inhibition of Rho kinase 17046269
Unchecked IC50 = 218.78 nM 6.66 Inhibition of ROCK 20347188

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

Data from ChEMBL 36 via Core Engine