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Compound Detail

CHEMBL1213539

NILTUBACIN
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O=C(O)CCCCCCC(=O)Nc1ccc([C@H]2O[C@@H](CSc3nc(-c4ccccc4)c(-c4ccccc4)o3)C[C@@H](c3ccc(CO)cc3)O2)cc1

Basic Information

ChEMBL ID CHEMBL1213539
Name NILTUBACIN
Phase Preclinical
Structure Type MOL
InChI Key WLLKRNCIQXOQHG-YXQOSMAKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

706.9
MW (Da)
9.20
ALogP
8
HBA
3
HBD
131.1
PSA (Ų)
0.07
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H42N2O7S
MW 706.86
Aromatic Rings 5
Heavy Atoms 51
NP-Likeness -0.28

Activity Summary

Ki 2 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 8
CHEMBL3192
Ki 6.12 6.12 750.0 1
Histone deacetylase 6
CHEMBL1865
Ki 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 8 Ki = 750.0 nM 6.12 Activity of human HDAC8 20139990
Histone deacetylase 6 Ki = 2200.0 nM 5.66 Inhibition of human HDAC6 20139990

Literature References

PubMed DOI Target Context # Activities
20139990 10.1038/nchembio.313 Histone deacetylase 6 1
20139990 10.1038/nchembio.313 Histone deacetylase 8 1

Data from ChEMBL 36 via Core Engine