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Compound Detail

CHEMBL1258747

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COc1ccc(C2CC(c3cc4ccccc4oc3=O)=NN2C(C)=O)cc1

Basic Information

ChEMBL ID CHEMBL1258747
Phase Preclinical
Structure Type MOL
InChI Key PCIIJXPELZPHAW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
3.50
ALogP
5
HBA
0
HBD
72.1
PSA (Ų)
0.67
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N2O4
MW 362.39
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.71

Activity Summary

IC50 4 meas. best 6.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 2
CHEMBL4102
IC50 6.39 6.39 410.0 1
Unchecked
CHEMBL612545
IC50 4.92 4.92 12000.0 1
Prostaglandin G/H synthase 1
CHEMBL2949
IC50 4.65 4.65 22400.0 1
Telomerase reverse transcriptase
CHEMBL2916
IC50 4.43 4.43 36700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30996860 10.1039/C8MD00457A Erythrocyte 10
30996860 10.1039/C8MD00457A ADMET 8
30996860 10.1039/C8MD00457A Rattus norvegicus 7
30996860 10.1039/C8MD00457A Unchecked 3
20800480 10.1016/j.bmcl.2010.08.017 SGC-7901 1
20800480 10.1016/j.bmcl.2010.08.017 PC-3 1
20800480 10.1016/j.bmcl.2010.08.017 A-431 1
20800480 10.1016/j.bmcl.2010.08.017 DNA polymerase I, thermostable 1
20800480 10.1016/j.bmcl.2010.08.017 Telomerase reverse transcriptase 1
30996860 10.1039/C8MD00457A Prostaglandin G/H synthase 1 1
30996860 10.1039/C8MD00457A Prostaglandin G/H synthase 2 1

Data from ChEMBL 36 via Core Engine