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Compound Detail

CHEMBL4873811

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CN1CCN(c2nc(-c3ccc(C(=O)NO)cc3)nc3cc(Cl)ccc23)CC1

Basic Information

ChEMBL ID CHEMBL4873811
Phase Preclinical
Structure Type MOL
InChI Key DYZSQWJEPPEPAQ-UHFFFAOYSA-N
8
Targets
8
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

397.9
MW (Da)
2.82
ALogP
6
HBA
2
HBD
81.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20ClN5O2
MW 397.87
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.59

Activity Summary

IC50 8 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 7.25 7.25 56.0 1
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 6.87 6.87 133.7 1
Histone deacetylase 1
CHEMBL325
IC50 6.44 6.44 359.4 1
Histone deacetylase 2
CHEMBL1937
IC50 6.43 6.43 374.3 1
Histone deacetylase 3
CHEMBL1829
IC50 6.38 6.38 414.1 1
MDA-MB-231
CHEMBL400
IC50 5.08 5.08 8400.0 1
MDA-MB-436
CHEMBL4296465
IC50 4.97 4.97 10600.0 1
MDA-MB-468
CHEMBL614335
IC50 4.84 4.84 14300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34139324 10.1016/j.bmcl.2021.128204 MDA-MB-231 28
34139324 10.1016/j.bmcl.2021.128204 Histone deacetylase 6 5
34139324 10.1016/j.bmcl.2021.128204 Serine/threonine-protein kinase mTOR 3
34139324 10.1016/j.bmcl.2021.128204 Histone deacetylase 1 2
34139324 10.1016/j.bmcl.2021.128204 Histone deacetylase 2 2
34139324 10.1016/j.bmcl.2021.128204 Histone deacetylase 3 2
34139324 10.1016/j.bmcl.2021.128204 MDA-MB-436 1
34139324 10.1016/j.bmcl.2021.128204 MDA-MB-468 1
34139324 10.1016/j.bmcl.2021.128204 MCF-10A 1
34139324 10.1016/j.bmcl.2021.128204 ADMET 1
34139324 10.1016/j.bmcl.2021.128204 No relevant target 1

Data from ChEMBL 36 via Core Engine