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Compound Detail

CHEMBL4635211

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Nc1ccc(F)cc1NC(=O)CCCCCNC(=O)c1cc(Cc2n[nH]c(=O)c3ccccc23)ccc1F

Basic Information

ChEMBL ID CHEMBL4635211
Phase Preclinical
Structure Type MOL
InChI Key UPODRFYFQLJARC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

519.5
MW (Da)
4.30
ALogP
5
HBA
4
HBD
130.0
PSA (Ų)
0.18
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27F2N5O3
MW 519.55
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 6.28 6.28 520.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 520.0 nM 6.28 Inhibition of HDAC1 (unknown origin) 32088129

Literature References

PubMed DOI Target Context # Activities
32088129 10.1016/j.bmcl.2020.127036 Poly [ADP-ribose] polymerase 1 1
32088129 10.1016/j.bmcl.2020.127036 Histone deacetylase 1 1
32088129 10.1016/j.bmcl.2020.127036 K562 1
32088129 10.1016/j.bmcl.2020.127036 MCF7 1
32088129 10.1016/j.bmcl.2020.127036 MDA-MB-231 1

Data from ChEMBL 36 via Core Engine