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Compound Detail

CHEMBL190525

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COc1ccccc1N1CCN(CCn2c(=O)[nH]c3cc(-c4ccc(C)cc4)[nH]c3c2=O)CC1

Basic Information

ChEMBL ID CHEMBL190525
Phase Preclinical
Structure Type MOL
InChI Key AGKWUSSOLCJWPA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
2.82
ALogP
6
HBA
2
HBD
86.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N5O3
MW 459.55
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.23

Activity Summary

Ki 2 meas. best 8.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.69 8.69 2.0 1
D(2) dopamine receptor
CHEMBL339
Ki 7.7 7.7 19.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15801833 10.1021/jm040870h Unchecked 2
15801833 10.1021/jm040870h Adrenergic receptor alpha-1 1
15801833 10.1021/jm040870h 5-hydroxytryptamine receptor 1A 1
15801833 10.1021/jm040870h D(1A) dopamine receptor 1
15801833 10.1021/jm040870h D(2) dopamine receptor 1
15801833 10.1021/jm040870h Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine