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Compound Detail

CHEMBL4537753

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Br.N#Cc1ccccc1-c1ccc(CN2C3=NCCCCN3c3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL4537753
Phase Preclinical
Structure Type MOL
InChI Key ZPLDATDRGRLRNA-UHFFFAOYSA-N
Parent Compound CHEMBL4594875
Active Moiety CHEMBL4594875
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

378.5
MW (Da)
5.20
ALogP
4
HBA
0
HBD
42.6
PSA (Ų)
0.63
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23BrN4
MW 459.39
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.06

Activity Summary

EC50 2 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1
CHEMBL2111345
EC50 6.36 6.355 440.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31358465 10.1016/j.bmcl.2019.07.035 AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 4
31358465 10.1016/j.bmcl.2019.07.035 No relevant target 2
31358465 10.1016/j.bmcl.2019.07.035 Peritoneal macrophage 2
31358465 10.1016/j.bmcl.2019.07.035 Unchecked 1
31358465 10.1016/j.bmcl.2019.07.035 Platelet 1
31358465 10.1016/j.bmcl.2019.07.035 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine