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Compound Detail

CHEMBL435806

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COC(=O)N1C[C@@]2(CC(C(=O)NC[C@H](NS(=O)(=O)c3c(C)cc(C)cc3C)C(=O)O)=NO2)C[C@H]1CNc1nc2ccccc2[nH]1

Basic Information

ChEMBL ID CHEMBL435806
Phase Preclinical
Structure Type MOL
InChI Key OMXIQNJVPRHGNN-IFCAXNDLSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

641.7
MW (Da)
1.80
ALogP
10
HBA
5
HBD
204.4
PSA (Ų)
0.22
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35N7O8S
MW 641.71
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.47

Activity Summary

IC50 4 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-5/beta-1
CHEMBL2095226
IC50 8.85 8.85 1.4 2
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 7.47 7.47 34.0 1
Integrin alpha-V/beta-1
CHEMBL2111407
IC50 7.47 7.47 34.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14698164 10.1016/j.bmcl.2003.10.057 Integrin alpha-V/beta-1 1
14698164 10.1016/j.bmcl.2003.10.057 Integrin alpha-V/beta-3 and alpha-IIb/beta 3 1
14698164 10.1016/j.bmcl.2003.10.057 Integrin alpha-5/beta-1 1
15974570 10.1021/jm040224i Integrin alpha-5/beta-1 1
15974570 10.1021/jm040224i Integrin alpha-V/beta-3 1
15974570 10.1021/jm040224i Integrin alpha-IIb/beta-3 1

Data from ChEMBL 36 via Core Engine