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Compound Detail

CHEMBL4875015

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Cl.Cn1cc(C(=O)Nc2ccc([C@@H]3C[C@H]3NCC3CC3)cc2)cn1

Basic Information

ChEMBL ID CHEMBL4875015
Phase Preclinical
Structure Type MOL
InChI Key XYFPAGOQZFSLFH-MCJVGQIASA-N
Parent Compound CHEMBL5029010
Active Moiety CHEMBL5029010
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

310.4
MW (Da)
2.53
ALogP
4
HBA
2
HBD
59.0
PSA (Ų)
0.86
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H23ClN4O
MW 346.86
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.75

Activity Summary

IC50 2 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LSD1/CoREST complex
CHEMBL3137262
IC50 8.68 8.68 2.1 1
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32931269 10.1021/acs.jmedchem.0c00919 Lysine-specific histone demethylase 1A 1
32931269 10.1021/acs.jmedchem.0c00919 LSD1/CoREST complex 1
32931269 10.1021/acs.jmedchem.0c00919 Amine oxidase [flavin-containing] A 1
32931269 10.1021/acs.jmedchem.0c00919 Amine oxidase [flavin-containing] B 1
- 10.6019/CHEMBL5724796 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5724796 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5724796 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5724796 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5724796 Aurora kinase A 1
- 10.6019/CHEMBL5724796 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5724796 Fibroblast growth factor receptor 2 1
- 10.6019/CHEMBL5724796 Peregrin 1
- 10.6019/CHEMBL5724796 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5724796 Bromodomain-containing protein 4 1

Data from ChEMBL 36 via Core Engine