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Compound Detail

CHEMBL3233432

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O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL3233432
Phase Preclinical
Structure Type MOL
InChI Key DLXKEWOEEPMPHX-PMACEKPBSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

380.5
MW (Da)
3.86
ALogP
4
HBA
0
HBD
32.8
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25FN2O2
MW 380.46
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.90

Activity Summary

Ki 7 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 9.05 9.05 0.9 1
D(2) dopamine receptor
CHEMBL339
Ki 7.39 7.39 41.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.98 6.98 104.0 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.58 6.58 262.0 1
D(4) dopamine receptor
CHEMBL219
Ki 6.5 6.5 320.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.28 6.28 520.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.88 5.88 1330.0 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