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Compound Detail

CHEMBL1224508

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COc1cc(C2CC(c3ccc(Br)cc3)=NN2C(C)=O)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL1224508
Phase Preclinical
Structure Type MOL
InChI Key HWVNVGUMBFMBCO-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

433.3
MW (Da)
4.17
ALogP
5
HBA
0
HBD
60.4
PSA (Ų)
0.71
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 C20H21BrN2O4
MW 433.30
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.69

Activity Summary

IC50 6 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
IMR-32
CHEMBL614585
IC50 5.5 5.5 3130.0 1
PC-3
CHEMBL390
IC50 5.46 5.46 3450.0 1
HEp-2
CHEMBL614735
IC50 5.34 5.34 4530.0 1
OVCAR
CHEMBL614212
IC50 5.32 5.32 4780.0 1
NCI-H460
CHEMBL396
IC50 5.22 5.22 6000.0 1
Xanthine dehydrogenase/oxidase
CHEMBL3649
IC50 4.13 4.13 74900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20702096 10.1016/j.bmc.2010.07.037 NCI-H460 1
21353569 10.1016/j.bmc.2011.01.058 Xanthine dehydrogenase/oxidase 1
- 10.1007/s00044-011-9824-9 HEp-2 1
- 10.1007/s00044-011-9824-9 IMR-32 1
- 10.1007/s00044-011-9824-9 OVCAR 1
- 10.1007/s00044-011-9824-9 PC-3 1
24835631 10.1016/j.bmcl.2014.04.094 Mycobacterium tuberculosis 1
24835631 10.1016/j.bmcl.2014.04.094 THP-1 1
24835631 10.1016/j.bmcl.2014.04.094 Unchecked 1

Data from ChEMBL 36 via Core Engine