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Compound Detail

CHEMBL387219

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O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1

Basic Information

ChEMBL ID CHEMBL387219
Phase Preclinical
Structure Type MOL
InChI Key FPVGIMJAYIADNO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

490.4
MW (Da)
3.81
ALogP
7
HBA
1
HBD
90.2
PSA (Ų)
0.58
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21F3N2O6
MW 490.43
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.02

Activity Summary

IC50 1 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
IC50 6.88 6.88 132.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanin-concentrating hormone receptor 1 IC50 = 132.0 nM 6.88 Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells 17064075

Literature References

PubMed DOI Target Context # Activities
17064075 10.1021/jm060683e Melanin-concentrating hormone receptor 1 2
17064075 10.1021/jm060683e Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine