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Compound Detail

CHEMBL337642

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O=C1NC(=O)C2=C1c1cn(c3ncccc13)CCOCCOCCOCCOCCn1cc2c2cccnc21

Basic Information

ChEMBL ID CHEMBL337642
Phase Preclinical
Structure Type MOL
InChI Key GJJAFPBCJBFVII-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

531.6
MW (Da)
2.03
ALogP
10
HBA
1
HBD
118.7
PSA (Ų)
0.34
QED
1
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N5O6
MW 531.57
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.36

Activity Summary

IC50 2 meas. best 7.47
EC50 1 meas. best 6.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 7.47 7.395 34.0 2
Unchecked
CHEMBL612545
EC50 6.41 6.41 390.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12954055 10.1021/jm030115o Unchecked 6
12954055 10.1021/jm030115o Mitogen-activated protein kinase 1 3
12954055 10.1021/jm030115o Glycogen synthase kinase-3 beta 2
12954055 10.1021/jm030115o Protein kinase C gamma type 2
12954055 10.1021/jm030115o Protein kinase C alpha type 2
12954055 10.1021/jm030115o Protein kinase C beta type 2
12954055 10.1021/jm030115o Protein kinase C theta type 2
12954055 10.1021/jm030115o CaM kinase II 2
15559249 10.1016/j.tips.2004.07.006 Glycogen synthase kinase-3 beta 1
12954055 10.1021/jm030115o Mitogen-activated protein kinase 9 1
12954055 10.1021/jm030115o Mitogen-activated protein kinase 10 1
12954055 10.1021/jm030115o MAP kinase-activated protein kinase 2 1
12954055 10.1021/jm030115o Dual specificity mitogen-activated protein kinase kinase 6 1
12954055 10.1021/jm030115o Ribosomal protein S6 kinase (P70S6K) 1
12954055 10.1021/jm030115o 3-phosphoinositide-dependent protein kinase 1 1
12954055 10.1021/jm030115o MAP kinase-activated protein kinase 5 1
12954055 10.1021/jm030115o Mitogen-activated protein kinase 8 1
12954055 10.1021/jm030115o Serine/threonine-protein kinase N2 1
12954055 10.1021/jm030115o Mitogen-activated protein kinase 11 1
12954055 10.1021/jm030115o Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine