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Compound Detail

CHEMBL513886

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CCO[C@@H](Cc1ccc(OCCN2CC=C(c3ccc(Cl)cc3)CC2)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL513886
Phase Preclinical
Structure Type MOL
InChI Key SBLZEXLDNURADT-QHCPKHFHSA-N
2
Targets
2
Activities
1
Assay Types
7
PK Parameters
5
Publications
0
Known Names

Molecular Properties

429.9
MW (Da)
4.54
ALogP
4
HBA
1
HBD
59.0
PSA (Ų)
0.60
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 C24H28ClNO4
MW 429.94
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.49

Activity Summary

EC50 2 meas. best 6.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 6.19 6.19 639.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 5.76 5.76 1730.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 116943.68 ng.hr.mL-1 Rattus norvegicus
AUC 116126.79 ng.hr.mL-1 Rattus norvegicus
CL 0.23 mL.min-1.kg-1 Rattus norvegicus
Cmax 15900.0 nM Rattus norvegicus
F 100.0 % Rattus norvegicus
T1/2 23.0 hr Rattus norvegicus
Tmax 0.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18771917 10.1016/j.bmcl.2008.08.020 Mus musculus 9
18771917 10.1016/j.bmcl.2008.08.020 Rattus norvegicus 8
18771917 10.1016/j.bmcl.2008.08.020 Peroxisome proliferator-activated receptor alpha 1
18771917 10.1016/j.bmcl.2008.08.020 Peroxisome proliferator-activated receptor gamma 1
18771917 10.1016/j.bmcl.2008.08.020 No relevant target 1

Data from ChEMBL 36 via Core Engine