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Compound Detail

CHEMBL5177494

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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)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL5177494
Phase Preclinical
Structure Type MOL
InChI Key CHQLJCSENLHOPW-ZQZJLAJUSA-N
4
Targets
7
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1319.6
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C64H86N16O11S2
MW 1319.63

Activity Summary

EC50 3 meas. best 8.29
Ki 3 meas. best 6.95
IC50 1 meas. best 4.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocyte-stimulating hormone receptor
CHEMBL3795
EC50 8.29 8.29 5.1 1
Melanocyte-stimulating hormone receptor
CHEMBL3795
Ki 6.95 6.95 112.2 1
Melanocortin receptor 3
CHEMBL4644
EC50 6.79 6.79 162.2 1
Melanocortin receptor 4
CHEMBL259
EC50 6.51 6.51 309.0 1
Melanocortin receptor 4
CHEMBL259
Ki 6.12 6.12 758.6 1
Melanocortin receptor 3
CHEMBL4644
Ki 5.01 5.01 9772.4 1
Melanocortin receptor 5
CHEMBL4608
IC50 4.68 4.68 20893.0 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