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Compound Detail

CHEMBL246794

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COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1

Basic Information

ChEMBL ID CHEMBL246794
Phase Preclinical
Structure Type MOL
InChI Key WTVQMTFZYWXSRS-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
4.94
ALogP
6
HBA
0
HBD
71.5
PSA (Ų)
0.40
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N3O5
MW 487.56
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.05

Activity Summary

Ki 5 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
Ki 6.79 6.79 164.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.48 6.48 330.0 1
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 6.43 6.43 370.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.06 6.06 880.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17448659 10.1016/j.bmcl.2007.04.012 Melanin-concentrating hormone receptor 1 2
17448659 10.1016/j.bmcl.2007.04.012 5-hydroxytryptamine receptor 2A 1
17448659 10.1016/j.bmcl.2007.04.012 5-hydroxytryptamine receptor 2C 1
17448659 10.1016/j.bmcl.2007.04.012 Muscarinic acetylcholine receptor M1 1
17448659 10.1016/j.bmcl.2007.04.012 Mus musculus 1
19290642 10.1021/jm8016199 Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine