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Compound Detail

CHEMBL3416055

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Cl.NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF

Basic Information

ChEMBL ID CHEMBL3416055
Phase Preclinical
Structure Type MOL
InChI Key XHNQQEONWOZBRI-SCYNACPDSA-N
Parent Compound CHEMBL3546907
Active Moiety CHEMBL3546907
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

243.7
MW (Da)
2.75
ALogP
2
HBA
1
HBD
35.2
PSA (Ų)
0.86
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 C12H16Cl2FNO
MW 280.17
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.30

Activity Summary

EC50 3 meas. best 7.5
IC50 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.5 7.5 32.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 6.2 6.2 632.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 5.83 5.83 1476.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25633969 10.1021/jm5019274 Salmonella typhimurium 8
25633969 10.1021/jm5019274 ADMET 3
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2A 2
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2B 2
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2C 2
25633969 10.1021/jm5019274 Nucleic Acid 2
25633969 10.1021/jm5019274 Plasma 2
25633969 10.1021/jm5019274 Brain 2
25633969 10.1021/jm5019274 Molecular identity unknown 1
25633969 10.1021/jm5019274 Mus musculus 1
25633969 10.1021/jm5019274 Voltage-gated inwardly rectifying potassium channel KCNH2 1
25633969 10.1021/jm5019274 Cytochrome P450 2B6 1
25633969 10.1021/jm5019274 Cytochrome P450 2C19 1
25633969 10.1021/jm5019274 Cytochrome P450 2C9 1
25633969 10.1021/jm5019274 Cytochrome P450 2D6 1
25633969 10.1021/jm5019274 Cytochrome P450 3A 1
25633969 10.1021/jm5019274 Liver 1
25633969 10.1021/jm5019274 Liver microsome 1

Data from ChEMBL 36 via Core Engine