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Compound Detail

CHEMBL1813011

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CCO[C@@H](Cc1ccc(OCCc2nc(-c3ccc(C)s3)oc2C)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL1813011
Phase Preclinical
Structure Type MOL
InChI Key KACYCSASEXQENA-IBGZPJMESA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

415.5
MW (Da)
4.67
ALogP
6
HBA
1
HBD
81.8
PSA (Ų)
0.52
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 C22H25NO5S
MW 415.51
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.94

Activity Summary

EC50 2 meas. best 10.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 10.74 10.74 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 455800.0 ng.hr.mL-1 Rattus norvegicus
Cmax 220692.64 nM Rattus norvegicus
T1/2 7.4 hr Rattus norvegicus
Tmax 0.667 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21450468 10.1016/j.bmcl.2011.03.020 Rattus norvegicus 76
21450468 10.1016/j.bmcl.2011.03.020 Mus musculus 26
21450468 10.1016/j.bmcl.2011.03.020 Peroxisome proliferator-activated receptor alpha 2
21450468 10.1016/j.bmcl.2011.03.020 Peroxisome proliferator-activated receptor gamma 2
21450468 10.1016/j.bmcl.2011.03.020 Peroxisome proliferator-activated receptor delta 1

Data from ChEMBL 36 via Core Engine