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Compound Detail

CHEMBL599994

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O=C(O)C(=O)N[C@H](Cc1ccc(OCC(=O)c2ccc(N3CCCC3)cc2)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL599994
Phase Preclinical
Structure Type MOL
InChI Key MXWXMANEMYOKGH-LJQANCHMSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

440.4
MW (Da)
1.74
ALogP
6
HBA
3
HBD
133.2
PSA (Ų)
0.40
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N2O7
MW 440.45
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.71

Activity Summary

IC50 3 meas. best 4.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 4A
CHEMBL5896
IC50 4.89 4.89 13000.0 1
Unchecked
CHEMBL612545
IC50 4.83 4.53 14800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lysine-specific demethylase 4A IC50 = 13000.0 nM 4.89 Inhibition of JMJD2A by MALDI-TOF assay 20088513
Unchecked IC50 = 14800.0 nM 4.83 Inhibition of JMJD2E by FDH coupled assay 20088513
Unchecked IC50 = 59000.0 nM 4.23 Inhibition of JMJD2E by MALDI-TOF assay 20088513

Literature References

PubMed DOI Target Context # Activities
20088513 10.1021/jm901680b Unchecked 4
20088513 10.1021/jm901680b Lysine-specific demethylase 4A 1

Data from ChEMBL 36 via Core Engine