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Compound Detail

CHEMBL316218

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Nc1nc(C[C@H](NC(=O)[C@H](Cc2ccccc2)NS(=O)(=O)N2CCOCC2)C(=O)N[C@@H](CC2CCCCC2)[C@@H](O)CC(=O)NCCN(CCO)CCO)cs1

Basic Information

ChEMBL ID CHEMBL316218
Phase Preclinical
Structure Type MOL
InChI Key XSBBDWMFZSROFA-YDPTYEFTSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

811.0
MW (Da)
-0.86
ALogP
13
HBA
8
HBD
248.8
PSA (Ų)
0.07
QED
3
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H58N8O9S2
MW 811.04
Aromatic Rings 2
Heavy Atoms 55
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.44 8.44 3.6 1
Cathepsin D
CHEMBL4106
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 3.61 nM 8.44 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 25000.0 nM 4.6 Inhibition of Bovine Cathepsin D 1635057

Literature References

PubMed DOI Target Context # Activities
1635057 10.1021/jm00092a006 Renin 1
1635057 10.1021/jm00092a006 Cathepsin D 1
1635057 10.1021/jm00092a006 Unchecked 1

Data from ChEMBL 36 via Core Engine