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Compound Detail

CHEMBL378151

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O=C(O)CC1CCCc2c1n(Cc1ccc(Cl)cc1)c1c(C(=O)Nc3ccccc3)cccc21

Basic Information

ChEMBL ID CHEMBL378151
Phase Preclinical
Structure Type MOL
InChI Key LSPSJQUSSWRPTE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

473.0
MW (Da)
6.49
ALogP
3
HBA
2
HBD
71.3
PSA (Ų)
0.34
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25ClN2O3
MW 472.97
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.71

Activity Summary

Ki 2 meas. best 7.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thromboxane A2 receptor
CHEMBL2069
Ki 7.06 7.06 88.0 1
Prostaglandin D2 receptor
CHEMBL4427
Ki 6.96 6.96 110.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thromboxane A2 receptor Ki = 88.0 nM 7.06 Binding affinity to TP receptor 16529930
Prostaglandin D2 receptor Ki = 110.0 nM 6.96 Binding affinity to DP receptor 16529930

Literature References

PubMed DOI Target Context # Activities
16529930 10.1016/j.bmcl.2006.02.062 Prostaglandin D2 receptor 1
16529930 10.1016/j.bmcl.2006.02.062 Thromboxane A2 receptor 1

Data from ChEMBL 36 via Core Engine