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Compound Detail

CHEMBL1743799

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Br.Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1

Basic Information

ChEMBL ID CHEMBL1743799
Phase Preclinical
Structure Type MOL
InChI Key AQKWUHDDUJOIFD-IDVLALEDSA-N
Parent Compound CHEMBL36416
Active Moiety CHEMBL36416
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

281.4
MW (Da)
3.38
ALogP
3
HBA
2
HBD
43.7
PSA (Ų)
0.79
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20BrNO2
MW 362.27
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.63

Activity Summary

Ki 5 meas. best 7.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Norepinephrine transporter
CHEMBL304
Ki 7.98 7.98 10.5 1
Sodium-dependent dopamine transporter
CHEMBL338
Ki 7.36 7.36 43.5 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.06 7.06 87.0 1
D(1A) dopamine receptor
CHEMBL265
Ki 6.97 6.97 106.0 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 6.91 6.91 124.0 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(1A) dopamine receptor 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
3039136 10.1021/jm00391a028 Serotonin 2 (5-HT2) receptor 1

Data from ChEMBL 36 via Core Engine