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Compound Detail

CHEMBL60610

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CC(C)C[C@H](O)[C@H](O)[C@H](CC1CCCCC1)NC(=O)[C@H](Cc1csc(N)n1)NC(=O)[C@@H]1Cc2ccccc2CN1S(=O)(=O)N1CCOCC1

Basic Information

ChEMBL ID CHEMBL60610
Phase Preclinical
Structure Type MOL
InChI Key DFJFFIIAHYRMCJ-STVCLKQXSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

721.0
MW (Da)
1.98
ALogP
10
HBA
5
HBD
187.4
PSA (Ų)
0.19
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H52N6O7S2
MW 720.96
Aromatic Rings 2
Heavy Atoms 49
NP-Likeness -0.51

Activity Summary

IC50 3 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.57 8.57 2.7 2
Cathepsin D
CHEMBL4106
IC50 4.52 4.52 30000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.7 nM 8.57 In vitro inhibition of monkey renin. 1635057
Renin IC50 = 2.71 nM 8.57 In vitro inhibitory activity against monkey plasma renin -
Cathepsin D IC50 = 30000.0 nM 4.52 Inhibition of Bovine Cathepsin D 1635057

Literature References

PubMed DOI Target Context # Activities
1635057 10.1021/jm00092a006 Monkey 3
1635057 10.1021/jm00092a006 Renin 1
1635057 10.1021/jm00092a006 Cathepsin D 1
1635057 10.1021/jm00092a006 Unchecked 1
- 10.1016/S0960-894X(01)80557-6 Renin 1

Data from ChEMBL 36 via Core Engine