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Compound Detail

CHEMBL5191916

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COc1cc(OC)cc(N(CCCCCCC(=O)NO)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL5191916
Phase Preclinical
Structure Type MOL
InChI Key SKDUGVKWEQCWQY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

504.6
MW (Da)
4.64
ALogP
9
HBA
2
HBD
114.6
PSA (Ų)
0.16
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N6O4
MW 504.59
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.04

Activity Summary

IC50 2 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 8.24 8.24 5.8 1
Histone deacetylase 6
CHEMBL1865
IC50 7.89 7.89 13.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 5.8 nM 8.24 Inhibition of HDAC1 (unknown origin) 36449947
Histone deacetylase 6 IC50 = 13.0 nM 7.89 Inhibition of HDAC6 (unknown origin) 36449947

Literature References

PubMed DOI Target Context # Activities
36449947 10.1021/acs.jmedchem.2c01413 Fibroblast growth factor receptor 1 3
36449947 10.1021/acs.jmedchem.2c01413 Histone deacetylase 1 1
36449947 10.1021/acs.jmedchem.2c01413 Histone deacetylase 6 1

Data from ChEMBL 36 via Core Engine