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Compound Detail

CHEMBL3978240

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COC(=O)[C@@H]1CNC[C@H](N(CC(C)C)C(=O)c2cnc(C(C)(C)C)nc2NCc2ccco2)C1

Basic Information

ChEMBL ID CHEMBL3978240
Phase Preclinical
Structure Type MOL
InChI Key XWKPQIHEQDPCKK-ZWKOTPCHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

471.6
MW (Da)
3.23
ALogP
8
HBA
2
HBD
109.6
PSA (Ų)
0.56
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H37N5O4
MW 471.60
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.33

Activity Summary

IC50 1 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.92 8.92 1.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 1.2 nM 8.92 Inhibition of recombinant human preprorenin expressed in human 293F cells using ... 27774132

Literature References

PubMed DOI Target Context # Activities
27774132 10.1021/acsmedchemlett.6b00251 Renin 2

Data from ChEMBL 36 via Core Engine