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Compound Detail

CHEMBL4127193

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O=C(NO)c1cccc2c1CN(c1nc3ccccc3[nH]1)C2

Basic Information

ChEMBL ID CHEMBL4127193
Phase Preclinical
Structure Type MOL
InChI Key WPCDPURYAICIPJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

294.3
MW (Da)
2.20
ALogP
4
HBA
3
HBD
81.2
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14N4O2
MW 294.31
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.06

Activity Summary

IC50 1 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 11
CHEMBL3310
IC50 6.77 6.77 170.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1118.38 ng.hr.mL-1 Mus musculus
CL 17.0 mL.min-1.g-1 Mus musculus
Cmax 4200.0 nM Mus musculus
F 81.0 % Mus musculus
T1/2 10.2 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29776742 10.1016/j.bmcl.2018.05.021 Mus musculus 4
29776742 10.1016/j.bmcl.2018.05.021 Histone deacetylase 11 1
29776742 10.1016/j.bmcl.2018.05.021 Histone deacetylase 6 1
29776742 10.1016/j.bmcl.2018.05.021 ADMET 1

Data from ChEMBL 36 via Core Engine