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Compound Detail

CHEMBL4757904

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O=C(C(CNC1CCCC1)c1ccc(Cl)cc1)N1CCN(c2ncnc3sc4c(c23)CCC4)CC1

Basic Information

ChEMBL ID CHEMBL4757904
Phase Preclinical
Structure Type MOL
InChI Key ITMQOKBFZDOCGE-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

510.1
MW (Da)
4.80
ALogP
6
HBA
1
HBD
61.4
PSA (Ų)
0.52
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32ClN5OS
MW 510.11
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.81

Activity Summary

IC50 7 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.47 7.47 34.0 1
Huh-7
CHEMBL614039
IC50 7.12 7.12 76.0 1
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
IC50 6.89 6.89 129.0 1
Hep 3B2
CHEMBL4296437
IC50 6.88 6.88 131.0 1
HepG2
CHEMBL395
IC50 6.74 6.74 183.0 1
SMMC-7721
CHEMBL613831
IC50 6.41 6.41 386.0 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 5.77 5.77 1710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32007668 10.1016/j.ejmech.2020.112076 Huh-7 36
32007668 10.1016/j.ejmech.2020.112076 Unchecked 5
32007668 10.1016/j.ejmech.2020.112076 RAC-beta serine/threonine-protein kinase 2
32007668 10.1016/j.ejmech.2020.112076 RAC-gamma serine/threonine-protein kinase 2
32007668 10.1016/j.ejmech.2020.112076 Hep 3B2 2
32007668 10.1016/j.ejmech.2020.112076 cAMP-dependent protein kinase catalytic subunit alpha 1
32007668 10.1016/j.ejmech.2020.112076 HepG2 1
32007668 10.1016/j.ejmech.2020.112076 SMMC-7721 1
32007668 10.1016/j.ejmech.2020.112076 Serine/threonine-protein kinase AKT 1
32007668 10.1016/j.ejmech.2020.112076 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine