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Compound Detail

CHEMBL4444654

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COc1ccc(CNCCCN2C(=O)c3ccc4c5c(ccc(c35)C2=O)C(=O)N(CCCNCc2ccc(OC)c(OC)c2OC)C4=O)c(OC)c1OC

Basic Information

ChEMBL ID CHEMBL4444654
Phase Preclinical
Structure Type MOL
InChI Key FCHFNNGGNLUVIH-UHFFFAOYSA-N
2
Targets
6
Activities
1
Assay Types
8
PK Parameters
6
Publications
0
Known Names

Molecular Properties

740.8
MW (Da)
4.44
ALogP
12
HBA
2
HBD
154.2
PSA (Ų)
0.11
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H44N4O10
MW 740.81
Aromatic Rings 4
Heavy Atoms 54
NP-Likeness -0.26

Activity Summary

IC50 6 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PC-3
CHEMBL390
IC50 6.2 6.0267 630.0 3
DU-145
CHEMBL613508
IC50 5.76 5.6233 1720.0 3

Pharmacokinetic Data

Parameter Value Units Species
Ka 4.3 10'-5/M -
Ka 4.2 10'-5/M -
Ka 17.11 10'-5/M -
Ka 18.9 10'-5/M -
Ka - - -
Ka - - -
Ka 15.71 10'-5/M -
Ka 7.06 10'-5/M -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31158753 10.1016/j.ejmech.2019.05.066 PC-3 16
31158753 10.1016/j.ejmech.2019.05.066 quadruplex DNA 15
31158753 10.1016/j.ejmech.2019.05.066 DU-145 11
31158753 10.1016/j.ejmech.2019.05.066 Mitogen-activated protein kinase; ERK1/ERK2 3
31158753 10.1016/j.ejmech.2019.05.066 Unchecked 3
31158753 10.1016/j.ejmech.2019.05.066 RAC-alpha serine/threonine-protein kinase 2

Data from ChEMBL 36 via Core Engine