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Compound Detail

CHEMBL4565367

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CC(C)[C@@H]1NC(=O)[C@H](CN)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 CHEMBL4565367
Phase Preclinical
Structure Type MOL
InChI Key ZJAPTWLOYMLZGR-WTBBZCIKSA-N
5
Targets
9
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

977.2
MW (Da)
-0.50
ALogP
10
HBA
10
HBD
303.1
PSA (Ų)
0.06
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C51H68N12O8
MW 977.18
Aromatic Rings 3
Heavy Atoms 71
NP-Likeness 0.55

Activity Summary

IC50 5 meas. best 8.09
Kd 4 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL3719
IC50 8.09 8.09 8.2 1
Melanocortin receptor 4
CHEMBL259
Kd 7.6 7.6 25.1 1
Melanocortin receptor 4
CHEMBL3719
Kd 7.5 7.5 31.6 1
Melanocortin receptor 4
CHEMBL259
IC50 7.49 7.49 32.2 1
Melanocortin receptor 5
CHEMBL4489
Kd 6.3 6.3 501.2 1
Melanocortin receptor 3
CHEMBL4774
Kd 6.1 6.1 794.3 1
Melanocortin receptor 5
CHEMBL4489
IC50 5.57 5.57 2700.0 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
IC50 5.1 5.1 8000.0 1
Melanocortin receptor 3
CHEMBL4774
IC50 5.0 5.0 10000.0 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