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Compound Detail

CHEMBL554267

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Cc1cc(C)c(S(=O)(=O)N[C@H](CNC(=O)c2coc(C)n2)C(=O)O)c(C)c1

Basic Information

ChEMBL ID CHEMBL554267
Phase Preclinical
Structure Type MOL
InChI Key LPYZHGQSYMJULB-CYBMUJFWSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

395.4
MW (Da)
1.07
ALogP
6
HBA
3
HBD
138.6
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21N3O6S
MW 395.44
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.98

Activity Summary

IC50 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V
CHEMBL3660
IC50 7.39 7.39 41.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.7 mL.min-1.kg-1 Rattus norvegicus
F 15.0 % Rattus norvegicus
Fu 0.049 - Rattus norvegicus
T1/2 7.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V IC50 = 41.0 nM 7.39 Inhibition of fibrinogen binding to alphavbeta3 integrin 19574045

Literature References

PubMed DOI Target Context # Activities
19574045 10.1016/j.bmcl.2009.06.041 Rattus norvegicus 4
19574045 10.1016/j.bmcl.2009.06.041 ADMET 3
19574045 10.1016/j.bmcl.2009.06.041 No relevant target 2
19574045 10.1016/j.bmcl.2009.06.041 Hepatocyte 1
19574045 10.1016/j.bmcl.2009.06.041 Plasma 1
19574045 10.1016/j.bmcl.2009.06.041 Integrin alpha-V 1

Data from ChEMBL 36 via Core Engine