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Compound Detail

CHEMBL1743820

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Br.COc1ccc([C@@H]2CN3CCC[C@@H]3c3ccccc32)cc1OC

Basic Information

ChEMBL ID CHEMBL1743820
Phase Preclinical
Structure Type MOL
InChI Key RAXSRZNGWGREMZ-CJRXIRLBSA-N
Parent Compound CHEMBL416595
Active Moiety CHEMBL416595
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

309.4
MW (Da)
3.99
ALogP
3
HBA
0
HBD
21.7
PSA (Ų)
0.86
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24BrNO2
MW 390.32
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness 0.13

Activity Summary

Ki 3 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Norepinephrine transporter
CHEMBL304
Ki 8.47 8.47 3.4 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 7.74 7.74 18.1 1
Sodium-dependent dopamine transporter
CHEMBL338
Ki 7.14 7.14 71.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3039136 10.1021/jm00391a028 Mus musculus 3
3039136 10.1021/jm00391a028 Sodium-dependent dopamine transporter 1
3039136 10.1021/jm00391a028 Norepinephrine transporter 1
3039136 10.1021/jm00391a028 Sodium-dependent serotonin transporter 1
3039136 10.1021/jm00391a028 D(2) dopamine receptor 1
3039136 10.1021/jm00391a028 Adrenergic receptor alpha-1 1
3039136 10.1021/jm00391a028 Adrenergic receptor alpha-2 1
3039136 10.1021/jm00391a028 Muscarinic acetylcholine receptor 1

Data from ChEMBL 36 via Core Engine