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Compound Detail

CHEMBL3233411

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CN1CCN2c3c(cccc31)[C@@H]1CN(CCCc3noc4ccccc34)CC[C@@H]12

Basic Information

ChEMBL ID CHEMBL3233411
Phase Preclinical
Structure Type MOL
InChI Key FINYFOYZAZLCFE-FPOVZHCZSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
3.89
ALogP
5
HBA
0
HBD
35.8
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O
MW 388.51
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.99

Activity Summary

Ki 5 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.48 8.48 3.3 1
D(2) dopamine receptor
CHEMBL339
Ki 6.76 6.76 174.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.54 6.54 287.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.53 6.53 294.0 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.5 6.5 314.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24559051 10.1021/jm401958n 5-hydroxytryptamine receptor 2A 1
24559051 10.1021/jm401958n 5-hydroxytryptamine receptor 2C 1
24559051 10.1021/jm401958n D(2) dopamine receptor 1
24559051 10.1021/jm401958n Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
24559051 10.1021/jm401958n Unchecked 1
24559051 10.1021/jm401958n Sodium-dependent serotonin transporter 1
24559051 10.1021/jm401958n 5-hydroxytryptamine receptor 1A 1
24559051 10.1021/jm401958n Histamine H1 receptor 1
24559051 10.1021/jm401958n Alpha-1A adrenergic receptor 1
24559051 10.1021/jm401958n Alpha-1B adrenergic receptor 1
24559051 10.1021/jm401958n D(1A) dopamine receptor 1
24559051 10.1021/jm401958n D(4) dopamine receptor 1
24559051 10.1021/jm401958n Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine