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Compound Detail

CHEMBL2179978

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Cl.N[C@H]1CCc2ccccc2[C@H](Sc2ccccc2)C1=O

Basic Information

ChEMBL ID CHEMBL2179978
Phase Preclinical
Structure Type MOL
InChI Key BRHNLLAQHHAIOC-NBLXOJGSSA-N
Parent Compound CHEMBL2220966
Active Moiety CHEMBL2220966
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

283.4
MW (Da)
3.36
ALogP
3
HBA
1
HBD
43.1
PSA (Ų)
0.86
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H18ClNOS
MW 319.86
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.05

Activity Summary

Ki 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL2590
Ki 7.22 7.22 60.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aminopeptidase N Ki = 60.0 nM 7.22 Competitive inhibition of pig APN using L-leucine-p-nitroanilide as substrate by... 22796349

Literature References

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

Data from ChEMBL 36 via Core Engine