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Compound Detail

CHEMBL435907

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

Basic Information

ChEMBL ID CHEMBL435907
Phase Preclinical
Structure Type MOL
InChI Key LRGIPQJRKVRNOS-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

409.9
MW (Da)
4.18
ALogP
5
HBA
1
HBD
67.6
PSA (Ų)
0.40
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20ClN3O3
MW 409.87
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.65

Activity Summary

IC50 7 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclooxygenase
CHEMBL2094253
IC50 7.52 7.52 30.0 1
Cyclooxygenase
CHEMBL2095157
IC50 7.52 7.16 30.0 2
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 6.96 6.96 110.0 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL312
IC50 6.96 6.025 110.0 2
Prostaglandin G/H synthase 1
CHEMBL2949
IC50 5.59 5.59 2540.0 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 6
10230624 10.1016/s0960-894x(99)00117-1 Polyunsaturated fatty acid 5-lipoxygenase 6
10230624 10.1016/s0960-894x(99)00117-1 Prostaglandin G/H synthase 1 1
16220969 10.1021/jm058225d Cyclooxygenase 1
16220969 10.1021/jm058225d Polyunsaturated fatty acid 5-lipoxygenase 1

Data from ChEMBL 36 via Core Engine