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Compound Detail

CHEMBL2324218

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C=CCOC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)NO)Cc1ccc2ccccc2c1

Basic Information

ChEMBL ID CHEMBL2324218
Phase Preclinical
Structure Type MOL
InChI Key RGXAXYLGCICSGR-PMACEKPBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

469.5
MW (Da)
1.37
ALogP
6
HBA
6
HBD
166.6
PSA (Ų)
0.05
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H31N5O5
MW 469.54
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 0.11

Activity Summary

Ki 1 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Insulin-degrading enzyme
CHEMBL1293287
Ki 5.28 5.28 5280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Insulin-degrading enzyme Ki = 5280.0 nM 5.28 Inhibition of human recombinant IDE-mediated FRET1 degradation 23437776

Literature References

PubMed DOI Target Context # Activities
23437776 10.1021/jm301280p Insulin-degrading enzyme 1

Data from ChEMBL 36 via Core Engine