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Compound Detail

CHEMBL1529613

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COc1ccc(C2CC(c3c(O)nc4ccc(Cl)cc4c3-c3ccccc3)=NN2C(=O)CCC(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL1529613
Phase Preclinical
Structure Type MOL
InChI Key UBBXFCINAAELSD-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

530.0
MW (Da)
5.81
ALogP
6
HBA
2
HBD
112.3
PSA (Ų)
0.31
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H24ClN3O5
MW 529.98
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.81

Activity Summary

IC50 5 meas. best 5.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL4117
IC50 5.31 5.31 4930.0 1
Glutamate receptor ionotropic, NMDA 2D
CHEMBL303
IC50 4.68 4.68 21000.0 1
Glutamate receptor ionotropic, NMDA 2C
CHEMBL401
IC50 4.55 4.55 28000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23909910 10.1021/jm400652r Unchecked 2
23909910 10.1021/jm400652r Glutamate receptor ionotropic, NMDA 2A 1
23909910 10.1021/jm400652r Glutamate receptor ionotropic, NMDA 2B 1
23909910 10.1021/jm400652r Glutamate receptor ionotropic, NMDA 2C 1
23909910 10.1021/jm400652r Glutamate receptor ionotropic, NMDA 2D 1
32037829 10.1021/acs.jmedchem.9b01526 DNA repair protein RAD51 homolog 1 1

Data from ChEMBL 36 via Core Engine