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Compound Detail

CHEMBL116055

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COc1ccc([C@H](CC(=O)O)NC(=O)CN2CC[C@H](CCc3ccc4c(n3)NCCC4)C2=O)cc1F

Basic Information

ChEMBL ID CHEMBL116055
Phase Preclinical
Structure Type MOL
InChI Key KBRCQTXEFPMTDE-UWJYYQICSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
2.70
ALogP
6
HBA
3
HBD
120.9
PSA (Ų)
0.46
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H31FN4O5
MW 498.56
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.55

Activity Summary

IC50 1 meas. best 9.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 9.31 9.31 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-3 IC50 = 0.49 nM 9.31 Inhibition of high affinity radioligand binding to human alphaV-beta3 integrin 11738567

Literature References

PubMed DOI Target Context # Activities
11738567 10.1016/s0960-894x(01)00666-7 Integrin alpha-V/beta-3 1
11738567 10.1016/s0960-894x(01)00666-7 Integrin alpha-IIb/beta-3 1
11738567 10.1016/s0960-894x(01)00666-7 No relevant target 1

Data from ChEMBL 36 via Core Engine