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Compound Detail

CHEMBL180489

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COc1ccc([C@@H](CCCCCCc2ccc3c(n2)NCCC3)CC(=O)O)cn1

Basic Information

ChEMBL ID CHEMBL180489
Phase Preclinical
Structure Type MOL
InChI Key SQIDFFKYMURYAR-SFHVURJKSA-N
2
Targets
3
Activities
1
Assay Types
6
PK Parameters
8
Publications
0
Known Names

Molecular Properties

397.5
MW (Da)
4.59
ALogP
5
HBA
2
HBD
84.3
PSA (Ų)
0.54
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H31N3O3
MW 397.52
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.10

Activity Summary

IC50 3 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 9.19 9.19 0.7 2
Unchecked
CHEMBL612545
IC50 7.41 7.41 39.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.0 mL.min-1.kg-1 Canis lupus familiaris
CL 5.1 mL.min-1.kg-1 Canis lupus familiaris
F 49.0 % Canis lupus familiaris
F 49.0 % Canis lupus familiaris
T1/2 9.0 hr Canis lupus familiaris
T1/2 9.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15369386 10.1021/jm049874c ADMET 4
15745815 10.1016/j.bmcl.2005.01.051 ADMET 3
15745815 10.1016/j.bmcl.2005.01.051 Integrin alpha-V/beta-3 2
15745815 10.1016/j.bmcl.2005.01.051 Unchecked 1
15745815 10.1016/j.bmcl.2005.01.051 Integrin alpha-IIb/beta-3 1
15745815 10.1016/j.bmcl.2005.01.051 No relevant target 1
15369386 10.1021/jm049874c Integrin alpha-V/beta-3 1
15369386 10.1021/jm049874c No relevant target 1

Data from ChEMBL 36 via Core Engine