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Compound Detail

CHEMBL5277547

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CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)O

Basic Information

ChEMBL ID CHEMBL5277547
Phase Preclinical
Structure Type MOL
InChI Key NSCMDQMHIHGCQG-NMTVEPIMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

766.9
MW (Da)
-3.56
ALogP
12
HBA
11
HBD
341.4
PSA (Ų)
0.05
QED
3
Ro5 Violations
23
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H54N10O11
MW 766.85
Aromatic Rings 1
Heavy Atoms 54
NP-Likeness 0.13

Activity Summary

IC50 2 meas. best 5.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PCSK9/LDLR
CHEMBL4523996
IC50 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PCSK9/LDLR IC50 = 1700.0 nM 5.77 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 3
36446632 10.1021/acs.jmedchem.2c01290 3-hydroxy-3-methylglutaryl-coenzyme A reductase 1

Data from ChEMBL 36 via Core Engine