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Compound Detail

CHEMBL1079339

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c1ccc(CCn2c(C3COc4ccccc4O3)nc3ccc(-c4ccncc4)cc32)cc1

Basic Information

ChEMBL ID CHEMBL1079339
Phase Preclinical
Structure Type MOL
InChI Key CRRZQPGSDPOHFI-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

433.5
MW (Da)
5.85
ALogP
5
HBA
0
HBD
49.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23N3O2
MW 433.51
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -0.66

Activity Summary

IC50 2 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.17 5.61 680.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 680.0 nM 6.17 Inhibition of ROCK by enzyme-coupled luciferase-kinase assay 20167489
Unchecked IC50 = 8810.0 nM 5.05 Inhibition of PKA 20167489

Literature References

PubMed DOI Target Context # Activities
20167489 10.1016/j.bmcl.2010.01.124 Unchecked 3
20167489 10.1016/j.bmcl.2010.01.124 Cytochrome P450 2C9 1
20167489 10.1016/j.bmcl.2010.01.124 Cytochrome P450 2D6 1
20167489 10.1016/j.bmcl.2010.01.124 Cytochrome P450 3A4 1
20167489 10.1016/j.bmcl.2010.01.124 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine