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Compound Detail

CHEMBL214178

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CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1

Basic Information

ChEMBL ID CHEMBL214178
Phase Preclinical
Structure Type MOL
InChI Key ISKBVCXTQANZNE-MHZLTWQESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.6
MW (Da)
4.05
ALogP
3
HBA
1
HBD
52.6
PSA (Ų)
0.61
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 C29H30FN3O2
MW 471.58
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.15

Activity Summary

Ki 1 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
Ki 6.84 6.84 145.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanin-concentrating hormone receptor 1 Ki = 145.0 nM 6.84 Functional antagonism of MCH-R1 expressed in HEK293 cells 17107791

Literature References

PubMed DOI Target Context # Activities
17107791 10.1016/j.bmcl.2006.10.053 5-hydroxytryptamine receptor 2C 1
17107791 10.1016/j.bmcl.2006.10.053 Voltage-gated inwardly rectifying potassium channel KCNH2 1
17107791 10.1016/j.bmcl.2006.10.053 Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine