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Compound Detail

CHEMBL142316

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O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL142316
Phase Preclinical
Structure Type MOL
InChI Key MFOZPYTUDQEMMW-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

412.5
MW (Da)
3.83
ALogP
5
HBA
0
HBD
53.8
PSA (Ų)
0.49
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29FN2O3
MW 412.51
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.55

Activity Summary

Kd 2 meas. best 6.23
Ki 2 meas. best 5.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL323
Kd 6.23 6.23 588.8 2
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.9 5.9 1258.9 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2A 2
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2B 1
11754579 10.1021/jm011014y 5-hydroxytryptamine receptor 2C 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2b (5HT2A and 5HT2B) 1
11754579 10.1021/jm011014y Serotonin receptor 2a and 2c (5HT2A and 5HT2C) 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2A 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2C 1
11101359 10.1021/jm0009890 D(1A) dopamine receptor 1
11101359 10.1021/jm0009890 D(2) dopamine receptor 1
11101359 10.1021/jm0009890 Unchecked 1
11101359 10.1021/jm0009890 Dopamine D2 receptor and serotonin 2a receptor 1
11101359 10.1021/jm0009890 5-hydroxytryptamine receptor 2B 1

Data from ChEMBL 36 via Core Engine