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Compound Detail

CHEMBL3775977

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O=c1[nH]cnc2c(-n3cc(CCN4CCC(c5ccc(Cl)cc5)CC4)cn3)nccc12

Basic Information

ChEMBL ID CHEMBL3775977
Phase Preclinical
Structure Type MOL
InChI Key SQDIBEJSOSAPGF-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

434.9
MW (Da)
3.58
ALogP
6
HBA
1
HBD
79.7
PSA (Ų)
0.52
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 C23H23ClN6O
MW 434.93
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.38

Activity Summary

IC50 5 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 5B
CHEMBL3774295
IC50 7.52 7.52 30.0 1
Lysine-specific demethylase 5C
CHEMBL2163176
IC50 7.17 7.17 67.0 1
Lysine-specific demethylase 4B
CHEMBL3313832
IC50 7.07 7.07 86.0 1
Lysine-specific demethylase 4A
CHEMBL5896
IC50 6.86 6.86 138.0 1
Lysine-specific demethylase 2A
CHEMBL1938210
IC50 5.17 5.17 6740.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26741168 10.1021/acs.jmedchem.5b01635 Lysine-specific demethylase 4A 1
26741168 10.1021/acs.jmedchem.5b01635 Lysine-specific demethylase 4B 1
26741168 10.1021/acs.jmedchem.5b01635 Lysine-specific demethylase 5B 1
26741168 10.1021/acs.jmedchem.5b01635 Lysine-specific demethylase 5C 1
26741168 10.1021/acs.jmedchem.5b01635 Lysine-specific demethylase 2A 1
26741168 10.1021/acs.jmedchem.5b01635 ADMET 1

Data from ChEMBL 36 via Core Engine