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Compound Detail

CHEMBL213255

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COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1

Basic Information

ChEMBL ID CHEMBL213255
Phase Preclinical
Structure Type MOL
InChI Key TVBZXJOQEZLHDL-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
5.09
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.56
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28N2O3
MW 416.52
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.22

Activity Summary

Ki 2 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
Ki 7.6 7.55 25.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.g-1 Rattus norvegicus
CL - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16839761 10.1016/j.bmcl.2006.06.056 Rattus norvegicus 2
16839761 10.1016/j.bmcl.2006.06.056 Melanin-concentrating hormone receptor 1 1
16839761 10.1016/j.bmcl.2006.06.056 Liver microsomes 1
17448659 10.1016/j.bmcl.2007.04.012 Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine