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Compound Detail

CHEMBL454025

DESCLASINOSE AZITHROMYCINARYLALKYL HYDROXAMATE
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CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)Cc3ccc(NC(=O)CCCCCCC(=O)NO)cc3)[C@H]2O)[C@](C)(O)C[C@@H](C)CN(C)[C@H](C)[C@@H](O)[C@]1(C)O

Basic Information

ChEMBL ID CHEMBL454025
Name DESCLASINOSE AZITHROMYCINARYLALKYL HYDROXAMATE
Phase Preclinical
Structure Type MOL
InChI Key DJGOCARXUHEYRZ-AYWHDHSOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

853.1
MW (Da)
3.33
ALogP
14
HBA
8
HBD
230.8
PSA (Ų)
0.06
QED
3
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H76N4O12
MW 853.11
Aromatic Rings 1
Heavy Atoms 60
NP-Likeness 0.99

Activity Summary

IC50 2 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase (HDAC1 and HDAC2)
CHEMBL2111429
IC50 6.96 6.96 109.8 1
Histone deacetylase 8
CHEMBL3192
IC50 5.63 5.63 2320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19093884 10.1021/jm801128g Histone deacetylase (HDAC1 and HDAC2) 1
19093884 10.1021/jm801128g Histone deacetylase 8 1
19093884 10.1021/jm801128g Unchecked 1
19093884 10.1021/jm801128g SK-MES-1 1
19093884 10.1021/jm801128g NCI-H69 1
19093884 10.1021/jm801128g DU-145 1
19093884 10.1021/jm801128g ADMET 1
19093884 10.1021/jm801128g HMEC 1

Data from ChEMBL 36 via Core Engine