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Compound Detail

CHEMBL3799094

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N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O

Basic Information

ChEMBL ID CHEMBL3799094
Phase Preclinical
Structure Type BOTH
InChI Key BBSFNUWKFPLIJR-JDRZNSOUSA-N
5
Targets
9
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1568.8
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C74H101N23O16
MW 1568.77

Activity Summary

EC50 6 meas. best 8.96
IC50 3 meas. best 6.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
EC50 8.96 7.39 1.1 2
Melanocortin receptor 5
CHEMBL4489
EC50 8.31 8.31 4.9 1
Melanocortin receptor 4
CHEMBL3719
EC50 7.84 7.84 14.5 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
EC50 7.79 7.79 16.4 1
Melanocortin receptor 3
CHEMBL4774
EC50 7.57 7.57 27.2 1
Melanocortin receptor 4
CHEMBL3719
IC50 6.59 6.59 258.0 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
IC50 5.96 5.96 1090.0 1
Melanocortin receptor 3
CHEMBL4774
IC50 5.07 5.07 8430.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 3 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocyte-stimulating hormone receptor 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 4 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 5 2
29669202 10.1021/acs.jmedchem.8b00238 Melanocortin receptor 4 2

Data from ChEMBL 36 via Core Engine