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Compound Detail

CHEMBL3741516

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O=C(/C=C/c1ccccc1)N1CCC(CN2CCC(c3noc4cc(F)ccc34)CC2)CC1

Basic Information

ChEMBL ID CHEMBL3741516
Phase Preclinical
Structure Type MOL
InChI Key ACVKASDZKIGIQP-RMKNXTFCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
5.10
ALogP
4
HBA
0
HBD
49.6
PSA (Ų)
0.51
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30FN3O2
MW 447.55
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.16

Activity Summary

Ki 1 meas. best 5.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.67 5.67 2115.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2A Ki = 2115.0 nM 5.67 Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00578C D(2) dopamine receptor 1
- 10.1039/C4MD00578C 5-hydroxytryptamine receptor 2A 1
- 10.1039/C4MD00578C 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine