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Compound Detail

CHEMBL1209915

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COc1ccc(C2CC(c3ccc(Br)cc3)=NN2C(C)=O)cc1

Basic Information

ChEMBL ID CHEMBL1209915
Phase Preclinical
Structure Type MOL
InChI Key NBLGDQOVNUSYKN-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
2
PK Parameters
12
Publications
0
Known Names

Molecular Properties

373.2
MW (Da)
4.16
ALogP
3
HBA
0
HBD
41.9
PSA (Ų)
0.81
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 C18H17BrN2O2
MW 373.25
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.13

Activity Summary

IC50 5 meas. best 4.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
IMR-32
CHEMBL614585
IC50 4.8 4.8 15670.0 1
OVCAR
CHEMBL614212
IC50 4.77 4.77 16870.0 1
PC-3
CHEMBL390
IC50 4.75 4.75 17780.0 1
HEp-2
CHEMBL614735
IC50 4.75 4.75 17870.0 1
Xanthine dehydrogenase/oxidase
CHEMBL3649
IC50 4.18 4.18 66500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 12.3 mL.min-1.g-1 Homo sapiens
CL 16.6 uL.min-1.(10^6cells)-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 2
20594840 10.1016/j.bmcl.2010.05.105 Bacillus subtilis 1
20594840 10.1016/j.bmcl.2010.05.105 Staphylococcus aureus 1
20594840 10.1016/j.bmcl.2010.05.105 Enterococcus faecalis 1
20594840 10.1016/j.bmcl.2010.05.105 Pseudomonas aeruginosa 1
20594840 10.1016/j.bmcl.2010.05.105 Escherichia coli 1
20594840 10.1016/j.bmcl.2010.05.105 Enterobacter cloacae 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

Data from ChEMBL 36 via Core Engine