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Compound Detail

CHEMBL3946540

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Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1

Basic Information

ChEMBL ID CHEMBL3946540
Phase Preclinical
Structure Type MOL
InChI Key QAJBOIGVHPCSNX-FQEVSTJZSA-N
12
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

372.9
MW (Da)
3.48
ALogP
4
HBA
0
HBD
24.9
PSA (Ų)
0.77
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 C21H25ClN2O2
MW 372.90
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.49

Activity Summary

Ki 12 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL2574
Ki 6.84 6.84 146.0 1
5-hydroxytryptamine receptor 2B
CHEMBL2583
Ki 6.26 6.26 551.0 1
5-hydroxytryptamine receptor 1A
CHEMBL3737
Ki 6.26 6.26 545.0 1
5-hydroxytryptamine receptor 1D
CHEMBL4297
Ki 5.95 5.95 1121.0 1
5-hydroxytryptamine receptor 2A
CHEMBL5377
Ki 5.89 5.89 1275.0 1
D(2) dopamine receptor
CHEMBL3427
Ki 5.72 5.72 1892.0 1
D(1A) dopamine receptor
CHEMBL3071
Ki 5.69 5.69 2041.0 1
5-hydroxytryptamine receptor 2C
CHEMBL3006
Ki 5.47 5.47 3386.0 1
Alpha-1D adrenergic receptor
CHEMBL2130
Ki 5.38 5.38 4181.0 1
Alpha-1B adrenergic receptor
CHEMBL2486
Ki 5.18 5.18 6637.0 1
D(3) dopamine receptor
CHEMBL3441
Ki 5.18 5.18 6645.0 1
Alpha-1A adrenergic receptor
CHEMBL2822
Ki 5.04 5.04 9037.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(4) dopamine receptor Ki = 146.0 nM 6.84 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 1A Ki = 545.0 nM 6.26 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2B Ki = 551.0 nM 6.26 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 1D Ki = 1121.0 nM 5.95 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2A Ki = 1275.0 nM 5.89 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(2) dopamine receptor Ki = 1892.0 nM 5.72 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(1A) dopamine receptor Ki = 2041.0 nM 5.69 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2C Ki = 3386.0 nM 5.47 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1D adrenergic receptor Ki = 4181.0 nM 5.38 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1B adrenergic receptor Ki = 6637.0 nM 5.18 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(3) dopamine receptor Ki = 6645.0 nM 5.18 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1A adrenergic receptor Ki = 9037.0 nM 5.04 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -

Data from ChEMBL 36 via Core Engine