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Compound Detail

CHEMBL4531291

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C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O

Basic Information

ChEMBL ID CHEMBL4531291
Phase Preclinical
Structure Type MOL
InChI Key XIDWPEYKZWKFNR-HPMMOBRVSA-N
5
Targets
8
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

930.1
MW (Da)
-0.44
ALogP
10
HBA
8
HBD
269.9
PSA (Ų)
0.11
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C49H59N11O8
MW 930.08
Aromatic Rings 4
Heavy Atoms 68
NP-Likeness 0.48

Activity Summary

IC50 5 meas. best 6.0
Kd 3 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Kd 6.4 6.4 398.1 1
Melanocortin receptor 4
CHEMBL3719
IC50 6.0 6.0 1000.0 1
Melanocortin receptor 4
CHEMBL3719
Kd 6.0 6.0 1000.0 1
Melanocortin receptor 4
CHEMBL259
IC50 5.57 5.57 2700.0 1
Melanocortin receptor 3
CHEMBL4774
Kd 5.4 5.4 3981.1 1
Melanocortin receptor 5
CHEMBL4489
IC50 4.92 4.92 12000.0 1
Melanocortin receptor 3
CHEMBL4774
IC50 4.82 4.82 15000.0 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
IC50 4.6 4.6 25000.0 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