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Compound Detail

CHEMBL3986651

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COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1

Basic Information

ChEMBL ID CHEMBL3986651
Phase Preclinical
Structure Type MOL
InChI Key ROKNCKQMECSPFV-NRFANRHFSA-N
12
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
2.84
ALogP
5
HBA
0
HBD
34.2
PSA (Ų)
0.75
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O3
MW 368.48
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.12

Activity Summary

Ki 12 meas. best 6.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL3737
Ki 6.76 6.76 174.0 1
5-hydroxytryptamine receptor 2B
CHEMBL2583
Ki 6.18 6.18 658.0 1
5-hydroxytryptamine receptor 2A
CHEMBL5377
Ki 5.85 5.85 1399.0 1
5-hydroxytryptamine receptor 1D
CHEMBL4297
Ki 5.7 5.7 1976.0 1
D(4) dopamine receptor
CHEMBL2574
Ki 5.47 5.47 3362.0 1
5-hydroxytryptamine receptor 2C
CHEMBL3006
Ki 5.42 5.42 3763.0 1
Alpha-1D adrenergic receptor
CHEMBL2130
Ki 5.19 5.19 6448.0 1
Alpha-1A adrenergic receptor
CHEMBL2822
Ki 5.08 5.08 8350.0 1
D(1A) dopamine receptor
CHEMBL3071
Ki 5.08 5.08 8366.0 1
D(3) dopamine receptor
CHEMBL3441
Ki 5.08 5.08 8286.0 1
D(1B) dopamine receptor
CHEMBL2737
Ki 5.07 5.07 8526.0 1
D(2) dopamine receptor
CHEMBL3427
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 1A Ki = 174.0 nM 6.76 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2B Ki = 658.0 nM 6.18 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2A Ki = 1399.0 nM 5.85 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 1D Ki = 1976.0 nM 5.7 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(4) dopamine receptor Ki = 3362.0 nM 5.47 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
5-hydroxytryptamine receptor 2C Ki = 3763.0 nM 5.42 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1D adrenergic receptor Ki = 6448.0 nM 5.19 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
Alpha-1A adrenergic receptor Ki = 8350.0 nM 5.08 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(1A) dopamine receptor Ki = 8366.0 nM 5.08 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(3) dopamine receptor Ki = 8286.0 nM 5.08 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(1B) dopamine receptor Ki = 8526.0 nM 5.07 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -
D(2) dopamine receptor Ki = 10000.0 nM 5.0 Radioligand Binding Assay: The detailed experimental protocols for the radioliga... -

Data from ChEMBL 36 via Core Engine