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Compound Detail

CHEMBL518665

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COC(=O)c1ccc2c(c1)CC(c1nc3ccc(-c4ccnc(N)n4)cc3o1)CO2

Basic Information

ChEMBL ID CHEMBL518665
Phase Preclinical
Structure Type MOL
InChI Key KFLADMPWLVWXMK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
3.37
ALogP
8
HBA
1
HBD
113.4
PSA (Ų)
0.52
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 C22H18N4O4
MW 402.41
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 2
CHEMBL2973
IC50 7.62 7.62 24.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase 2 IC50 = 24.0 nM 7.62 Inhibition of ROCK2 18996009

Literature References

PubMed DOI Target Context # Activities
18996009 10.1016/j.bmcl.2008.10.095 Rho-associated protein kinase 2 2
18996009 10.1016/j.bmcl.2008.10.095 Unchecked 1
18996009 10.1016/j.bmcl.2008.10.095 Liver microsomes 1

Data from ChEMBL 36 via Core Engine