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Compound Detail

CHEMBL5184950

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Nc1ncc(-c2cn(Cc3ccc(C(=O)NO)cc3)c(=O)c(Nc3ccccc3)n2)cn1

Basic Information

ChEMBL ID CHEMBL5184950
Phase Preclinical
Structure Type MOL
InChI Key NRUBHLGNOGYUOE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

429.4
MW (Da)
2.19
ALogP
9
HBA
4
HBD
148.1
PSA (Ų)
0.27
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19N7O3
MW 429.44
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.12

Activity Summary

IC50 1 meas. best 8.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 8.16 8.16 6.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 6 IC50 = 6.9 nM 8.16 Inhibition of HDAC6 (unknown origin) 36272186

Literature References

PubMed DOI Target Context # Activities
36272186 10.1016/j.bmc.2022.117067 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 2
36272186 10.1016/j.bmc.2022.117067 Histone deacetylase 6 2

Data from ChEMBL 36 via Core Engine