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Compound Detail

CHEMBL429882

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CC[C@H](C)[C@H](NC(=O)[C@H](C[C@H](O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)NC(CO)(CO)CO)C(C)C)C(=O)NCc1ccccn1

Basic Information

ChEMBL ID CHEMBL429882
Phase Preclinical
Structure Type MOL
InChI Key ZAWLRCAPIHLGNI-BPVPQGFMSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

977.2
MW (Da)
1.19
ALogP
12
HBA
10
HBD
291.5
PSA (Ų)
0.05
QED
3
Ro5 Violations
27
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C50H76N10O10
MW 977.22
Aromatic Rings 3
Heavy Atoms 70
NP-Likeness -0.18

Activity Summary

IC50 1 meas. best 9.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL2322
IC50 9.48 9.48 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.417 hr -
T1/2 0.5 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.33 nM 9.48 Tested in vitro for inhibitory activity against plasma renin in rat models 2197413

Literature References

PubMed DOI Target Context # Activities
2197413 10.1021/jm00170a036 Renin 3
2197413 10.1021/jm00170a036 ADMET 2
2197413 10.1021/jm00170a036 No relevant target 2

Data from ChEMBL 36 via Core Engine