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Compound Detail

CHEMBL4094606

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CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4094606
Phase Preclinical
Structure Type MOL
InChI Key DBJGVYJTQHCOAH-BAIHPJFXSA-N
4
Targets
7
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1667.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C76H111N23O16S2
MW 1667.00

Activity Summary

EC50 3 meas. best 7.38
Ki 3 meas. best 6.44
IC50 1 meas. best 5.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocyte-stimulating hormone receptor
CHEMBL3795
EC50 7.38 7.38 41.7 1
Melanocyte-stimulating hormone receptor
CHEMBL3795
Ki 6.44 6.44 363.1 1
Melanocortin receptor 3
CHEMBL4644
EC50 5.67 5.67 2138.0 1
Melanocortin receptor 4
CHEMBL259
EC50 5.51 5.51 3090.3 1
Melanocortin receptor 5
CHEMBL4608
IC50 5.39 5.39 4073.8 1
Melanocortin receptor 3
CHEMBL4644
Ki 4.63 4.63 23442.3 1
Melanocortin receptor 4
CHEMBL259
Ki 4.6 4.6 25118.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29605997 10.1021/acs.jmedchem.8b00170 Melanocortin receptor 4 6
29605997 10.1021/acs.jmedchem.8b00170 Melanocyte-stimulating hormone receptor 4
29605997 10.1021/acs.jmedchem.8b00170 Melanocortin receptor 3 4
29605997 10.1021/acs.jmedchem.8b00170 Melanocortin receptor 5 2
29605997 10.1021/acs.jmedchem.8b00170 No relevant target 1

Data from ChEMBL 36 via Core Engine