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Compound Detail

CHEMBL3946661

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c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1

Basic Information

ChEMBL ID CHEMBL3946661
Phase Preclinical
Structure Type MOL
InChI Key ZKTUDHGKQCWRDH-FQEVSTJZSA-N
13
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
2.83
ALogP
4
HBA
0
HBD
24.9
PSA (Ų)
0.81
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 C21H26N2O2
MW 338.45
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.17

Activity Summary

Ki 13 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL3737
Ki 9.22 9.22 0.6 1
D(4) dopamine receptor
CHEMBL2574
Ki 6.88 6.88 132.0 1
D(2) dopamine receptor
CHEMBL3427
Ki 6.47 6.47 342.0 1
5-hydroxytryptamine receptor 7
CHEMBL4764
Ki 6.33 6.33 468.0 1
5-hydroxytryptamine receptor 1D
CHEMBL4297
Ki 6.23 6.23 590.0 1
5-hydroxytryptamine receptor 2A
CHEMBL5377
Ki 6.09 6.09 817.0 1
D(1A) dopamine receptor
CHEMBL3071
Ki 5.87 5.87 1353.0 1
5-hydroxytryptamine receptor 2B
CHEMBL2583
Ki 5.84 5.84 1445.0 1
Alpha-1D adrenergic receptor
CHEMBL2130
Ki 5.64 5.64 2307.0 1
Alpha-1A adrenergic receptor
CHEMBL2822
Ki 5.57 5.57 2720.0 1
D(3) dopamine receptor
CHEMBL3441
Ki 5.55 5.55 2827.0 1
5-hydroxytryptamine receptor 2C
CHEMBL3006
Ki 5.17 5.17 6736.0 1
Alpha-1B adrenergic receptor
CHEMBL2486
Ki 5.14 5.14 7211.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 1A Ki = 0.6 nM 9.22 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(4) dopamine receptor Ki = 132.0 nM 6.88 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(2) dopamine receptor Ki = 342.0 nM 6.47 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 7 Ki = 468.0 nM 6.33 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 1D Ki = 590.0 nM 6.23 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2A Ki = 817.0 nM 6.09 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(1A) dopamine receptor Ki = 1353.0 nM 5.87 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2B Ki = 1445.0 nM 5.84 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1D adrenergic receptor Ki = 2307.0 nM 5.64 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1A adrenergic receptor Ki = 2720.0 nM 5.57 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(3) dopamine receptor Ki = 2827.0 nM 5.55 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2C Ki = 6736.0 nM 5.17 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1B adrenergic receptor Ki = 7211.0 nM 5.14 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -

Data from ChEMBL 36 via Core Engine