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Compound Detail

CHEMBL4127829

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Cc1nc(N2Cc3cccc(C(=O)NO)c3C2)[nH]c1C

Basic Information

ChEMBL ID CHEMBL4127829
Phase Preclinical
Structure Type MOL
InChI Key APXXOQCOOOYNJR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

272.3
MW (Da)
1.67
ALogP
4
HBA
3
HBD
81.2
PSA (Ų)
0.57
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 C14H16N4O2
MW 272.31
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 11
CHEMBL3310
IC50 5.64 5.64 2300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 88.0 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 11 IC50 = 2300.0 nM 5.64 Inhibition of full length recombinant human HDAC11 expressed in baculoviral expr... 29776742

Literature References

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

Data from ChEMBL 36 via Core Engine