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Compound Detail

CHEMBL14362

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COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cnccc3C)c1)CC2

Basic Information

ChEMBL ID CHEMBL14362
Phase Preclinical
Structure Type MOL
InChI Key JPJZJSNUFFGCEC-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

461.9
MW (Da)
6.33
ALogP
3
HBA
1
HBD
54.5
PSA (Ų)
0.50
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19ClF3N3O2
MW 461.87
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.38

Activity Summary

IC50 1 meas. best 4.96
Ki 1 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 9.2 9.2 0.6 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
10737744 10.1021/jm990388c Serotonin receptor (2b and 2c) 1
10737744 10.1021/jm990388c Cytochrome P450 1A2 1
10737744 10.1021/jm990388c Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine