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Compound Detail

CHEMBL5094892

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CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O)C(C)C)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL5094892
Phase Preclinical
Structure Type MOL
InChI Key QJDIGHNKOUHIAO-PBIDRDJCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

1623.8
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C77H106N16O23
MW 1623.78

Activity Summary

IC50 1 meas. best 4.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PCSK9/LDLR
CHEMBL4523996
IC50 4.57 4.57 27120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PCSK9/LDLR IC50 = 27120.0 nM 4.57 Inhibition of PCSK9-LDLR (unknown origin) protein-protein interaction 36446632

Literature References

PubMed DOI Target Context # Activities
36446632 10.1021/acs.jmedchem.2c01290 PCSK9/LDLR 2
36446632 10.1021/acs.jmedchem.2c01290 Proprotein convertase subtilisin/kexin type 9 2
34266235 10.1021/acs.jmedchem.0c02051 HepG2 1

Data from ChEMBL 36 via Core Engine