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Compound Detail

CHEMBL4166675

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O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1

Basic Information

ChEMBL ID CHEMBL4166675
Phase Preclinical
Structure Type MOL
InChI Key HWLBVPZMVBRPLK-KJXAQDMKSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
3.44
ALogP
3
HBA
1
HBD
66.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17F3N2O3
MW 438.41
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 0.25

Activity Summary

EC50 2 meas. best 7.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
EC50 7.03 7.03 93.3 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29704723 10.1016/j.ejmech.2018.04.020 Histamine H3 receptor 4
29704723 10.1016/j.ejmech.2018.04.020 5-hydroxytryptamine receptor 2C 2
29704723 10.1016/j.ejmech.2018.04.020 Histamine H1 receptor 2
29704723 10.1016/j.ejmech.2018.04.020 Histamine H2 receptor 2
29704723 10.1016/j.ejmech.2018.04.020 Histamine H4 receptor 2
29704723 10.1016/j.ejmech.2018.04.020 Luciferin 4-monooxygenase 1
29704723 10.1016/j.ejmech.2018.04.020 HEK-293T 1
29704723 10.1016/j.ejmech.2018.04.020 No relevant target 1

Data from ChEMBL 36 via Core Engine