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Compound Detail

CHEMBL5182345

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CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL5182345
Phase Preclinical
Structure Type MOL
InChI Key MWUXCBIVLGSGOO-INFFCAIZSA-N
4
Targets
7
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1243.5
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C58H82N16O11S2
MW 1243.53

Activity Summary

EC50 3 meas. best 8.32
Ki 3 meas. best 7.24
IC50 1 meas. best 5.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocyte-stimulating hormone receptor
CHEMBL3795
EC50 8.32 8.32 4.8 1
Melanocortin receptor 4
CHEMBL259
EC50 7.32 7.32 47.9 1
Melanocyte-stimulating hormone receptor
CHEMBL3795
Ki 7.24 7.24 57.5 1
Melanocortin receptor 3
CHEMBL4644
EC50 6.72 6.72 190.6 1
Melanocortin receptor 4
CHEMBL259
Ki 6.53 6.53 295.1 1
Melanocortin receptor 5
CHEMBL4608
IC50 5.38 5.38 4168.7 1
Melanocortin receptor 3
CHEMBL4644
Ki 5.2 5.2 6309.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36167503 10.1021/acs.jmedchem.2c00793 Unchecked 4
36167503 10.1021/acs.jmedchem.2c00793 Melanocyte-stimulating hormone receptor 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 3 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 4 2
36167503 10.1021/acs.jmedchem.2c00793 Melanocortin receptor 5 1

Data from ChEMBL 36 via Core Engine