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Compound Detail

CHEMBL1819542

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CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL1819542
Phase Preclinical
Structure Type BOTH
InChI Key DHMCDFJJCGVQSC-OVCMMVBBSA-N
4
Targets
8
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

992.2
MW (Da)
-4.62
ALogP
15
HBA
12
HBD
405.3
PSA (Ų)
0.06
QED
3
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H65N13O11S2
MW 992.20
Aromatic Rings 1
Heavy Atoms 68
NP-Likeness 0.39

Activity Summary

EC50 8 meas. best 9.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V1a receptor
CHEMBL2868
EC50 9.92 9.915 0.1 2
Vasopressin V1a receptor
CHEMBL1889
EC50 9.57 9.57 0.3 2
Vasopressin V1b receptor
CHEMBL1921
EC50 7.6 7.6 25.0 2
Vasopressin V2 receptor
CHEMBL1790
EC50 6.81 6.81 154.9 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21688787 10.1021/jm200278m Vasopressin V1a receptor 4
21688787 10.1021/jm200278m Unchecked 2
21688787 10.1021/jm200278m Vasopressin V1b receptor 2
21688787 10.1021/jm200278m Vasopressin V2 receptor 2
21688787 10.1021/jm200278m Oxytocin receptor 2
21688787 10.1021/jm200278m Rattus norvegicus 1
21688787 10.1021/jm200278m Vasopressin V1a/V2 1

Data from ChEMBL 36 via Core Engine