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Compound Detail

CHEMBL211742

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COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1

Basic Information

ChEMBL ID CHEMBL211742
Phase Preclinical
Structure Type MOL
InChI Key RBPXZGGCEYINEX-HHHXNRCGSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

584.5
MW (Da)
4.13
ALogP
6
HBA
2
HBD
86.8
PSA (Ų)
0.33
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35Cl2N5O3
MW 584.55
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.26

Activity Summary

Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Ki 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3500.0 mL.min-1.kg-1 Rattus norvegicus
F - % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 4 Ki = 10.0 nM 8.0 Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells 16697187

Literature References

PubMed DOI Target Context # Activities
16697187 10.1016/j.bmcl.2006.04.069 Rattus norvegicus 1
16697187 10.1016/j.bmcl.2006.04.069 Liver microsomes 1
16697187 10.1016/j.bmcl.2006.04.069 Melanocortin receptor 4 1

Data from ChEMBL 36 via Core Engine