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Compound Detail

CHEMBL378016

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Cc1[nH]c2ccccc2c1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1

Basic Information

ChEMBL ID CHEMBL378016
Phase Preclinical
Structure Type MOL
InChI Key WQMKKOKOWWDFGB-DEOSSOPVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
5.82
ALogP
3
HBA
2
HBD
65.4
PSA (Ų)
0.43
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H35F3N4O
MW 500.61
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.99

Activity Summary

Ki 1 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Ki 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 4 Ki = 1600.0 nM 5.8 Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells 16777413

Literature References

PubMed DOI Target Context # Activities
16777413 10.1016/j.bmcl.2006.05.088 Melanocortin receptor 4 1

Data from ChEMBL 36 via Core Engine