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Compound Detail

CHEMBL516203

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O=C1Nc2nc(-c3c(O)cccc3OCC3CC3)cc([C@@H]3CCCNC3)c2CO1

Basic Information

ChEMBL ID CHEMBL516203
Phase Preclinical
Structure Type MOL
InChI Key IGJVFGZEWDGDOO-CQSZACIVSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

395.5
MW (Da)
3.77
ALogP
6
HBA
3
HBD
92.7
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N3O4
MW 395.46
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.12

Activity Summary

Ki 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
Ki 8.7 8.7 2.0 1
Unchecked
CHEMBL612545
Ki 8.7 7.785 2.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 HEK-293T 8
- 10.6019/CHEMBL5303304 U2OS 6
33481605 10.1021/acs.jmedchem.0c01511 Unchecked 2
19285872 10.1016/j.bmc.2009.02.041 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
- 10.6019/CHEMBL3301361 ADMET 1
- 10.6019/CHEMBL5303304 Fibroblast 1
- 10.6019/CHEMBL5308504 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5308504 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5308504 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5308504 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5308504 Aurora kinase A 1
- 10.6019/CHEMBL5308504 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5308504 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5308504 Peregrin 1
- 10.6019/CHEMBL5308504 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5308504 Bromodomain-containing protein 4 1

Data from ChEMBL 36 via Core Engine