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Compound Detail

CHEMBL3349030

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CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O

Basic Information

ChEMBL ID CHEMBL3349030
Phase Preclinical
Structure Type BOTH
InChI Key GZWUQPQBOGLSIM-DNTYTYIFSA-N
3
Targets
34
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

1570.8
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C74H99N21O16S
MW 1570.80

Activity Summary

EC50 17 meas. best 8.7
IC50 17 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 3
CHEMBL4644
EC50 8.7 7.3371 2.0 7
Melanocortin receptor 4
CHEMBL259
EC50 8.44 6.988 3.6 5
Melanocortin receptor 3
CHEMBL4644
IC50 8.06 6.46 8.8 6
Melanocortin receptor 4
CHEMBL259
IC50 8.01 6.442 9.7 5
Melanocortin receptor 5
CHEMBL4608
EC50 7.31 6.166 49.0 5
Melanocortin receptor 5
CHEMBL4608
IC50 7.11 5.9 77.0 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 3 EC50 = 2.0 nM 8.7 Effective concentration required for intracellular cAMP accumulation against Mel... 11150170
Melanocortin receptor 4 EC50 = 3.6 nM 8.44 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 3 IC50 = 8.8 nM 8.06 Binding affinity for Human Melanocortin 3 receptor expressed in L-cells 11150170
Melanocortin receptor 4 IC50 = 9.7 nM 8.01 Binding affinity for Human Melanocortin 4 receptor expressed in L-cells 11150170
Melanocortin receptor 3 EC50 = 11.0 nM 7.96 Effective concentration required for intracellular cAMP accumulation against Mel... 11150170
Melanocortin receptor 3 EC50 = 12.0 nM 7.92 Effective concentration required for intracellular cAMP accumulation against Mel... 11150170
Melanocortin receptor 3 EC50 = 35.0 nM 7.46 Effective concentration required for intracellular cAMP accumulation against Mel... 11150170
Melanocortin receptor 3 EC50 = 42.0 nM 7.38 Effective concentration required for intracellular cAMP accumulation against Mel... 11150170
Melanocortin receptor 5 EC50 = 49.0 nM 7.31 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 5 IC50 = 77.0 nM 7.11 Binding affinity for Human Melanocortin 5 receptor expressed in L-cells 11150170
Melanocortin receptor 4 EC50 = 190.0 nM 6.72 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 4 EC50 = 190.0 nM 6.72 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 4 EC50 = 190.0 nM 6.72 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 3 IC50 = 280.0 nM 6.55 Binding affinity for Human Melanocortin 3 receptor expressed in L-cells 11150170
Melanocortin receptor 3 IC50 = 340.0 nM 6.47 Binding affinity for Human Melanocortin 3 receptor expressed in L-cells 11150170
Melanocortin receptor 5 IC50 = 350.0 nM 6.46 Binding affinity for Human Melanocortin 5 receptor expressed in L-cells 11150170
Melanocortin receptor 4 IC50 = 430.0 nM 6.37 Binding affinity for Human Melanocortin 4 receptor expressed in L-cells 11150170
Melanocortin receptor 4 EC50 = 460.0 nM 6.34 Effective concentration required for intracellular cAMP accumulation by Melanoco... 11150170
Melanocortin receptor 3 IC50 = 470.0 nM 6.33 Binding affinity for Human Melanocortin 3 receptor expressed in L-cells 11150170
Melanocortin receptor 3 IC50 = 610.0 nM 6.21 Binding affinity for Human Melanocortin 3 receptor expressed in L-cells 11150170

Literature References

PubMed DOI Target Context # Activities
11150170 10.1021/jm000211e Melanocortin receptor 3 21
11150170 10.1021/jm000211e Melanocortin receptor 4 17
11150170 10.1021/jm000211e Melanocortin receptor 5 17

Data from ChEMBL 36 via Core Engine