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Compound Detail

CHEMBL56608

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CC(C)C[C@H](NC(=O)CC(O)C(CC1CCCCC1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)NCc1cccc(CN=C(N)N)c1

Basic Information

ChEMBL ID CHEMBL56608
Phase Preclinical
Structure Type MOL
InChI Key RJHLUHRYEJUXPP-WRVQWQNJSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

873.1
MW (Da)
3.40
ALogP
9
HBA
9
HBD
268.0
PSA (Ų)
0.05
QED
2
Ro5 Violations
22
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H68N10O7
MW 873.11
Aromatic Rings 3
Heavy Atoms 63
NP-Likeness 0.02

Activity Summary

IC50 3 meas. best 9.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.23 8.71 0.6 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.59 nM 9.23 Inhibition of renin 3050088
Renin IC50 = 1.4 nM 8.85 Concentration required for 50% inhibition of human plasma renin 3050088
Renin IC50 = 9.0 nM 8.05 Inhibition of porcine kidney renin 3050088

Literature References

PubMed DOI Target Context # Activities
3050088 10.1021/jm00118a009 No relevant target 3
3050088 10.1021/jm00118a009 Renin 3

Data from ChEMBL 36 via Core Engine