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Compound Detail

CHEMBL5273040

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C=C/C(O[C@H](C)C(=O)NCC(=O)NCC(=O)O)=c1/c2c(c(=O)oc1=C)CCC2

Basic Information

ChEMBL ID CHEMBL5273040
Phase Preclinical
Structure Type MOL
InChI Key FCSFQXYKHFZUTC-YOEHMKRZSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
-1.44
ALogP
6
HBA
3
HBD
134.9
PSA (Ų)
0.49
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22N2O7
MW 390.39
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.31

Activity Summary

EC50 4 meas. best 6.27
IC50 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 5A
CHEMBL2424504
IC50 7.62 7.62 24.0 1
MDA-MB-231
CHEMBL400
EC50 6.27 6.27 540.0 1
MDA-MB-468
CHEMBL614335
EC50 6.15 6.15 710.0 1
MCF7
CHEMBL387
EC50 5.65 5.65 2260.0 1
Lysine-specific demethylase 5C
CHEMBL2163176
IC50 5.22 5.22 6030.0 1
MCF-10A
CHEMBL614321
EC50 5.09 5.09 8210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34555614 10.1016/j.ejmech.2021.113855 MDA-MB-231 1
34555614 10.1016/j.ejmech.2021.113855 MDA-MB-468 1
34555614 10.1016/j.ejmech.2021.113855 Lysine-specific demethylase 5A 1
34555614 10.1016/j.ejmech.2021.113855 Lysine-specific demethylase 5C 1
34555614 10.1016/j.ejmech.2021.113855 MCF7 1
34555614 10.1016/j.ejmech.2021.113855 MCF-10A 1
34555614 10.1016/j.ejmech.2021.113855 L02 1

Data from ChEMBL 36 via Core Engine