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Compound Detail

CHEMBL3753740

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O=C(O)CCNc1nc(N2CCc3ccccc3CC2)cc(-n2nccn2)n1

Basic Information

ChEMBL ID CHEMBL3753740
Phase Preclinical
Structure Type MOL
InChI Key QVJZTXXAWSJFPD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

379.4
MW (Da)
1.55
ALogP
8
HBA
2
HBD
109.1
PSA (Ų)
0.66
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21N7O2
MW 379.42
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.13

Activity Summary

IC50 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 6B
CHEMBL1938211
IC50 6.57 6.57 270.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.0 mL.min-1.g-1 Homo sapiens
T1/2 38.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26776360 10.1016/j.bmcl.2016.01.006 Liver microsome 2
26776360 10.1016/j.bmcl.2016.01.006 Lysine-specific demethylase 6B 1
26776360 10.1016/j.bmcl.2016.01.006 Cytochrome P450 3A4 1
26776360 10.1016/j.bmcl.2016.01.006 Cytochrome P450 2D6 1
26776360 10.1016/j.bmcl.2016.01.006 Cytochrome P450 2C9 1
26776360 10.1016/j.bmcl.2016.01.006 Cytochrome P450 1A2 1
26776360 10.1016/j.bmcl.2016.01.006 Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine