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Compound Detail

CHEMBL175372

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COc1ccc(-n2nc(C#CC(C)N(O)C(=O)c3cccnc3)cc2-c2ccc(C)cc2)cc1

Basic Information

ChEMBL ID CHEMBL175372
Phase Preclinical
Structure Type MOL
InChI Key CUUSTGBVBGDOHQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
4.52
ALogP
6
HBA
1
HBD
80.5
PSA (Ų)
0.27
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N4O3
MW 452.51
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.78

Activity Summary

IC50 3 meas. best 5.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 1
CHEMBL2949
IC50 5.22 5.22 6000.0 1
Cyclooxygenase
CHEMBL2095157
IC50 4.94 4.94 11500.0 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL312
IC50 4.59 4.59 25400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10230624 10.1016/s0960-894x(99)00117-1 Cyclooxygenase 2
10230624 10.1016/s0960-894x(99)00117-1 Polyunsaturated fatty acid 5-lipoxygenase 2
10230624 10.1016/s0960-894x(99)00117-1 Prostaglandin G/H synthase 1 1

Data from ChEMBL 36 via Core Engine