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Compound Detail

CHEMBL3216892

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Cl.Cl.O=C1Nc2cc(Br)ccc2/C1=C1/Nc2ccccc2/C1=N\OCCN1CCN(CCO)CC1

Basic Information

ChEMBL ID CHEMBL3216892
Phase Preclinical
Structure Type MOL
InChI Key DLXPXTHNXDDQNS-GMWAXMIDSA-N
Parent Compound CHEMBL522503
Active Moiety CHEMBL522503
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

512.4
MW (Da)
2.57
ALogP
7
HBA
3
HBD
89.4
PSA (Ų)
0.31
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28BrCl2N5O3
MW 585.33
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.30

Activity Summary

IC50 4 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.38 7.54 4.2 2
Cyclin-dependent kinase 1/cyclin B1
CHEMBL1907602
IC50 6.4 6.4 400.0 1
SH-SY5Y
CHEMBL614910
IC50 4.78 4.78 16700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27726390 10.1021/acs.jnatprod.6b00285 KCL-22 4
18816110 10.1021/jm800648y No relevant target 3
18816110 10.1021/jm800648y Unchecked 2
18816110 10.1021/jm800648y Cyclin-dependent kinase 1/cyclin B1 1
18816110 10.1021/jm800648y SH-SY5Y 1

Data from ChEMBL 36 via Core Engine