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Compound Detail

CHEMBL435323

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CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL435323
Phase Preclinical
Structure Type MOL
InChI Key KEBRFHAVFOSSOX-WSFLLCRESA-N
6
Targets
10
Activities
3
Assay Types
2
PK Parameters
20
Publications
0
Known Names

Molecular Properties

1040.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H65N13O11S2
MW 1040.24

Activity Summary

Kd 5 meas. best 7.03
EC50 3 meas. best 10.3
Ki 2 meas. best 9.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V2 receptor
CHEMBL1790
EC50 10.3 10.3 0.1 1
Vasopressin V2 receptor
CHEMBL3766
Ki 9.59 9.59 0.3 1
Vasopressin V1b receptor
CHEMBL1921
EC50 7.62 7.62 24.0 1
Rattus norvegicus
CHEMBL376
Kd 7.03 7.03 93.3 5
Vasopressin V1a receptor
CHEMBL2868
Ki 6.5 6.5 316.0 1
Oxytocin receptor
CHEMBL2049
EC50 6.46 6.46 350.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 9.6 mL.min-1.kg-1 Rattus norvegicus
CL - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2909737 10.1021/jm00121a043 Rattus norvegicus 6
31022340 10.1021/acs.jmedchem.9b00132 ADMET 3
6892930 10.1021/jm00178a003 Rattus norvegicus 3
926126 10.1021/jm00219a026 Rattus norvegicus 3
926117 10.1021/jm00219a012 Rattus norvegicus 3
950656 10.1021/jm00228a023 Rattus norvegicus 3
628009 10.1021/jm00201a019 Rattus norvegicus 2
950656 10.1021/jm00228a023 Oxytocin receptor 2
926117 10.1021/jm00219a012 NON-PROTEIN TARGET 2
17300166 10.1021/jm060928n Rattus norvegicus 2
722751 10.1021/jm00207a002 Rattus norvegicus 2
31022340 10.1021/acs.jmedchem.9b00132 Oxytocin receptor 2
31022340 10.1021/acs.jmedchem.9b00132 Vasopressin V1b receptor 2
31022340 10.1021/acs.jmedchem.9b00132 Unchecked 2
17300166 10.1021/jm060928n Vasopressin V1a receptor 1
17300166 10.1021/jm060928n Vasopressin V2 receptor 1
17300166 10.1021/jm060928n Oxytocin receptor 1
926126 10.1021/jm00219a026 NON-PROTEIN TARGET 1
31022340 10.1021/acs.jmedchem.9b00132 Vasopressin V2 receptor 1
31022340 10.1021/acs.jmedchem.9b00132 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine