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Compound Detail

CHEMBL323839

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COc1ccc(C[C@H](NC(=O)C(C)(C)N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CC2CCCCC2)[C@@H](O)[C@@H](O)CC(C)C)cc1

Basic Information

ChEMBL ID CHEMBL323839
Phase Preclinical
Structure Type MOL
InChI Key UGXKCYZOKRDKII-VFFRCKCKSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

642.8
MW (Da)
2.13
ALogP
8
HBA
7
HBD
191.7
PSA (Ų)
0.14
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H54N6O6
MW 642.84
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness 0.31

Activity Summary

Ki 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
Ki 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 0.5 % Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin Ki = 14.0 nM 7.85 Binding affinity against aspartic protease renin. 10669559

Literature References

PubMed DOI Target Context # Activities
10669559 10.1021/jm990412m ADMET 1
10669559 10.1021/jm990412m Renin 1

Data from ChEMBL 36 via Core Engine