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Compound Detail

CHEMBL4785157

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CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C1=O

Basic Information

ChEMBL ID CHEMBL4785157
Phase Preclinical
Structure Type MOL
InChI Key KRKOVWQTFADIDL-BUXPKPHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

977.1
MW (Da)
-1.27
ALogP
10
HBA
9
HBD
311.4
PSA (Ų)
0.06
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C50H64N12O9
MW 977.14
Aromatic Rings 3
Heavy Atoms 71
NP-Likeness 0.39

Activity Summary

EC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocyte-stimulating hormone receptor
CHEMBL4077
EC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocyte-stimulating hormone receptor EC50 = 1000.0 nM 6.0 Agonist activity at mouse MC1R by alphascreen cAMP assay 33062177

Literature References

PubMed DOI Target Context # Activities
33062177 10.1021/acsmedchemlett.9b00641 Melanocortin receptor 3 2
33062177 10.1021/acsmedchemlett.9b00641 Melanocortin receptor 4 2
33062177 10.1021/acsmedchemlett.9b00641 Melanocyte-stimulating hormone receptor 1
33062177 10.1021/acsmedchemlett.9b00641 Melanocortin receptor 5 1

Data from ChEMBL 36 via Core Engine