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Compound Detail

CHEMBL3416047

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C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL3416047
Phase Preclinical
Structure Type MOL
InChI Key BVQUTZSFPJRZCS-XQKZEKTMSA-N
Parent Compound CHEMBL3546973
Active Moiety CHEMBL3546973
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

237.7
MW (Da)
2.97
ALogP
2
HBA
1
HBD
35.2
PSA (Ų)
0.80
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 C15H17ClF3NO3
MW 351.75
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.07

Activity Summary

EC50 2 meas. best 7.22
IC50 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 7.22 7.22 60.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 6.57 6.57 270.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 5.66 5.66 2211.0 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 2C 2
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2B 2
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
25633969 10.1021/jm5019274 Unchecked 1
25633969 10.1021/jm5019274 5-hydroxytryptamine receptor 2A 1
25633969 10.1021/jm5019274 Molecular identity unknown 1

Data from ChEMBL 36 via Core Engine