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Compound Detail

CHEMBL4786329

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CCOC(=O)CCNc1cc(N2CCc3ccccc3CC2)nc(-c2cccnc2)n1

Basic Information

ChEMBL ID CHEMBL4786329
Phase Preclinical
Structure Type MOL
InChI Key LQPGVGSKBNXQDU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
3.51
ALogP
7
HBA
1
HBD
80.2
PSA (Ų)
0.59
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C24H27N5O2
MW 417.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.50

Activity Summary

IC50 1 meas. best 4.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 2B
CHEMBL3779760
IC50 4.62 4.62 24000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lysine-specific demethylase 2B IC50 = 24000.0 nM 4.62 Inhibition of KDM2B (1 to 650 residues)(unknown origin) by Alphalisa assay 25279926

Literature References

PubMed DOI Target Context # Activities
22842901 10.1038/nature11262 Macrophage 73
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4689842 U2OS 9
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4689842 HEK-293T 9
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
22842901 10.1038/nature11262 Unchecked 4
25279926 10.1038/nature13688 Lysine-specific demethylase 4C 2
25279926 10.1038/nature13688 Lysine-specific demethylase 6B 2
22842901 10.1038/nature11262 Lysine-specific demethylase 6B 2
- 10.6019/CHEMBL5060014 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5060014 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5209897 Lysine-specific demethylase 6A 1
- 10.6019/CHEMBL5060014 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5060014 Casein kinase I isoform delta 1
25279926 10.1038/nature13688 Lysine-specific demethylase 2B 1
- 10.6019/CHEMBL5060014 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5060014 Bromodomain-containing protein 4 1

Data from ChEMBL 36 via Core Engine