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Compound Detail

CHEMBL137719

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c1ccc(C(OCCC2CCN(Cc3cccnc3)CC2)c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL137719
Phase Preclinical
Structure Type MOL
InChI Key ACUBOAOOZIDJOY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

386.5
MW (Da)
5.49
ALogP
3
HBA
0
HBD
25.4
PSA (Ų)
0.51
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N2O
MW 386.54
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.77

Activity Summary

IC50 2 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL338
IC50 7.31 7.31 48.6 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 6.17 6.17 680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
9016326 10.1021/jm960638e Sodium-dependent dopamine transporter 1
9016326 10.1021/jm960638e Sodium-dependent serotonin transporter 1
9016326 10.1021/jm960638e Monoamine transporters; serotonin & dopamine 1
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1

Data from ChEMBL 36 via Core Engine