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Compound Detail

CHEMBL1668623

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Cl.NC1Cc2ccccc2CC1=O

Basic Information

ChEMBL ID CHEMBL1668623
Phase Preclinical
Structure Type MOL
InChI Key NPDBUWUEHWAHRS-UHFFFAOYSA-N
Parent Compound CHEMBL1739274
Active Moiety CHEMBL1739274
1
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

161.2
MW (Da)
0.68
ALogP
2
HBA
1
HBD
43.1
PSA (Ų)
0.61
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H12ClNO
MW 197.66
Aromatic Rings 1
Heavy Atoms 12
NP-Likeness 0.50

Activity Summary

Ki 3 meas. best 6.3
IC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL1907
Ki 6.3 6.3 500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aminopeptidase N Ki = 500.0 nM 6.3 Inhibition of human aminopeptidase N by Dixon plot analysis 21292493
Aminopeptidase N Ki = 500.0 nM 6.3 Inhibition of APN 22796349

Literature References

PubMed DOI Target Context # Activities
21292493 10.1016/j.bmc.2011.01.008 Aminopeptidase N 3
22796349 10.1016/j.bmc.2012.06.041 Aminopeptidase N 2
21292493 10.1016/j.bmc.2011.01.008 Cytosol aminopeptidase 1
21292493 10.1016/j.bmc.2011.01.008 Leukotriene A-4 hydrolase 1
21292493 10.1016/j.bmc.2011.01.008 Unchecked 1
22796349 10.1016/j.bmc.2012.06.041 Cytosol aminopeptidase 1

Data from ChEMBL 36 via Core Engine