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Compound Detail

CHEMBL373343

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COc1cccc(OC)c1-c1ccc(C[C@@H](Cn2oc(=O)[nH]c2=O)NC(=O)[C@@H]2CCCN2S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc1

Basic Information

ChEMBL ID CHEMBL373343
Phase Preclinical
Structure Type MOL
InChI Key XCYVGOOLNFZXSG-UPVQGACJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

677.6
MW (Da)
3.70
ALogP
9
HBA
2
HBD
152.9
PSA (Ų)
0.24
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30Cl2N4O8S
MW 677.56
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness -0.82

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-4/beta-1
CHEMBL1907599
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-4/beta-1 IC50 = 6.0 nM 8.22 Inhibition of VLA-4 receptor of Jurkat cells in BURJ assay 16039122

Literature References

PubMed DOI Target Context # Activities
16039122 10.1016/j.bmcl.2005.06.034 Integrin alpha-4/beta-1 1

Data from ChEMBL 36 via Core Engine