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Compound Detail

CHEMBL157757

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C=C(C)c1ccc(CN2CCC(CCOC(c3ccccc3)c3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL157757
Phase Preclinical
Structure Type MOL
InChI Key CBTZWAGMSGXAIF-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
7.13
ALogP
2
HBA
0
HBD
12.5
PSA (Ų)
0.36
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35NO
MW 425.62
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.36

Activity Summary

IC50 4 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 8.51 8.51 3.1 1
Sodium-dependent dopamine transporter
CHEMBL338
IC50 7.94 7.94 11.6 1
Norepinephrine transporter
CHEMBL304
IC50 6.08 6.08 832.0 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 5.99 5.99 1030.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11806716 10.1021/jm010316x Sodium-dependent dopamine transporter 1
11806716 10.1021/jm010316x Sodium-dependent serotonin transporter 1
11806716 10.1021/jm010316x Norepinephrine transporter 1
11806716 10.1021/jm010316x Rattus norvegicus 1
11806716 10.1021/jm010316x Monoamine transporters; serotonin & dopamine 1
11806716 10.1021/jm010316x Monoamine transporters; Norepininephrine & dopamine 1
11806716 10.1021/jm010316x Unchecked 1

Data from ChEMBL 36 via Core Engine