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Compound Detail

CHEMBL4538274

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CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O

Basic Information

ChEMBL ID CHEMBL4538274
Phase Preclinical
Structure Type MOL
InChI Key LPATVOINCAVXRL-NTBYCYSFSA-N
5
Targets
9
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

1005.2
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H68N12O9
MW 1005.19

Activity Summary

IC50 5 meas. best 7.42
Kd 4 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Kd 7.8 7.8 15.8 1
Melanocortin receptor 4
CHEMBL3719
IC50 7.42 7.42 38.0 1
Melanocortin receptor 4
CHEMBL3719
Kd 7.2 7.2 63.1 1
Melanocortin receptor 4
CHEMBL259
IC50 6.6 6.6 250.0 1
Melanocortin receptor 5
CHEMBL4489
Kd 6.1 6.1 794.3 1
Melanocortin receptor 3
CHEMBL4774
Kd 5.9 5.9 1258.9 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
IC50 4.82 4.82 15000.0 1
Melanocortin receptor 5
CHEMBL4489
IC50 4.54 4.54 29000.0 1
Melanocortin receptor 3
CHEMBL4774
IC50 4.28 4.28 53000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31845801 10.1021/acs.jmedchem.9b00860 Melanocortin receptor 4 8
31845801 10.1021/acs.jmedchem.9b00860 Melanocortin receptor 3 4
31845801 10.1021/acs.jmedchem.9b00860 Melanocortin receptor 5 4
31845801 10.1021/acs.jmedchem.9b00860 Melanocyte-stimulating hormone receptor 3

Data from ChEMBL 36 via Core Engine