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Compound Detail

CHEMBL14352

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COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2

Basic Information

ChEMBL ID CHEMBL14352
Phase Preclinical
Structure Type MOL
InChI Key ROZXAOHUYCQNLS-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

337.3
MW (Da)
3.70
ALogP
3
HBA
1
HBD
54.5
PSA (Ų)
0.91
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 C16H14F3N3O2
MW 337.30
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.64

Activity Summary

Ki 4 meas. best 8.0
IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 8.0 8.0 10.0 2
Cytochrome P450 1A2
CHEMBL3356
IC50 7.7 7.7 20.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.0 6.0 1000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9572885 10.1021/jm970741j Rattus norvegicus 17
10737744 10.1021/jm990388c Serotonin 2 receptors; 5-HT2a & 5-HT2c 2
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2A 1
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2B 1
10737744 10.1021/jm990388c 5-hydroxytryptamine receptor 2C 1
10737744 10.1021/jm990388c Cytochrome P450 1A2 1
10737744 10.1021/jm990388c Rattus norvegicus 1
9572885 10.1021/jm970741j 5-hydroxytryptamine receptor 2A 1
9572885 10.1021/jm970741j 5-hydroxytryptamine receptor 2C 1
9572885 10.1021/jm970741j Serotonin 2 receptors; 5-HT2a & 5-HT2c 1

Data from ChEMBL 36 via Core Engine