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Compound Detail

CHEMBL540357

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Br.N=C(N)SCCCn1cc(C2=C(Nc3ccccc3)C(=O)NC2=O)c2ccccc21

Basic Information

ChEMBL ID CHEMBL540357
Phase Preclinical
Structure Type MOL
InChI Key FJQLQQSUKIIOJC-UHFFFAOYSA-N
Parent Compound CHEMBL1190211
Active Moiety CHEMBL1190211
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
3.14
ALogP
6
HBA
4
HBD
113.0
PSA (Ų)
0.20
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22BrN5O2S
MW 500.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.75

Activity Summary

IC50 5 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C beta type
CHEMBL3045
IC50 8.7 8.6967 2.0 3
Protein kinase C alpha type
CHEMBL299
IC50 7.57 7.57 27.0 1
Protein kinase C epsilon type
CHEMBL3582
IC50 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1007/s00044-010-9439-6 Protein kinase C beta type 2
15380221 10.1016/j.bmcl.2004.07.061 Protein kinase C beta type 1
15380221 10.1016/j.bmcl.2004.07.061 Protein kinase C alpha type 1
15380221 10.1016/j.bmcl.2004.07.061 Protein kinase C epsilon type 1

Data from ChEMBL 36 via Core Engine