General Information of the Compound
Compound ID
CP0042717
Compound Name
(buspirone) 8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione
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Synonyms
8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione
8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione
8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione
8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
Ansial
Ansial (TN)
Ansiced
Ansiced (TN)
Anxiron
Anxiron (TN)
Axoren
Axoren (TN)
Bespar
Bespar (TN)
BuSpar (TN)
Buspimen (TN)
Buspinol (TN)
Buspiron (TN)
Buspirona
Buspirona [INN-Spanish]
Buspirone
Buspirone (INN)
Buspirone [INN:BAN]
Buspirone-MDTS
Buspironum
Buspironum [INN-Latin]
Buspisal
Buspisal (TN)
Gen-Buspirone
Gen-Buspirone (TN)
MJ-9022-1
N-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1-cyclopentanediacetamide
Narol (TN)
Sorbon (TN)
Spamilan (TN)
Spitomin (TN)
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Structure
Formula
C21H31N5O2
Molecular Weight
385.512
Canonical SMILES
O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
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InChI
InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2
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InChIKey
QWCRAEMEVRGPNT-UHFFFAOYSA-N
CAS
36505-84-7
Physicochemical Property
logP
2.0882
Rotatable Bonds
6
Heavy Atom Count
28
Polar Areas
69.64
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Complexity
28

"RO5" indicates the cutoff set by lipinski's rule of five:

(1) Molecular weight less than 500 Dalton;

(2) xlogp less than 5;

(3) No more than 5 hbonddonor (Hydrogen Bond Donor Count);

(4) No more than 10 hbondacc (Hydrogen Bond Acceptor Count);

(5) No more than 10 rotbonds (Rotatable Bond Count).

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Click to Show/Hide the External Link(s) of This Compound
PubChem ID
CID: 2477
SID: 14902734
ChEMBL ID
CHEMBL49
DrugBank ID
DB00490
Map of Molecular Bioactivity Related to the Compound
Map of Molecular Bioactivity Related to the Compound

Compound
Cell Line
Protein

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Compound
Protein ID: PT00819, 5-hydroxytryptamine receptor 1A
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000026 CHO-K1 Cricetulus griseus (Chinese hamster)  5
1
EC50 = 15.14 nM
   TI
   LI
   LO
   TS
2
EC50 = 38.02 nM
   TI
   LI
   LO
   TS
3
EC50 = 72.44 nM
   TI
   LI
   LO
   TS
4
Ki = 5.012 nM
   TI
   LI
   LO
   TS
5
Ki = 21 nM
   TI
   LI
   LO
   TS
CL000011 CHO Cricetulus griseus (Chinese hamster)  2
1
EC50 = 41 nM
   TI
   LI
   LO
   TS
2
Ki = 20 nM
   TI
   LI
   LO
   TS
CL000043 U2OS Homo sapiens (Human)  1
1
EC50 = 186.21 nM
   TI
   LI
   LO
   TS
CL000006 HEK293 Homo sapiens (Human)  6
1
Ki = 12 nM
   TI
   LI
   LO
   TS
2
Ki = 20 nM
   TI
   LI
   LO
   TS
3
Ki = 21 nM
   TI
   LI
   LO
   TS
4
Ki = 22 nM
   TI
   LI
   LO
   TS
5
Ki = 32.2 nM
   TI
   LI
   LO
   TS
6
Ki = 34.3 nM
   TI
   LI
   LO
   TS
CL000025 HEK-293T Homo sapiens (Human)  1
1
Ki = 50 nM
   TI
   LI
   LO
   TS
Biochemical Assays
1 IC50 = 25 nM
2 Kd = 10 nM
3 Ki = 4 nM
4 Ki = 4.78 nM
5 Ki = 15 nM
6 Ki = 17 nM
7 Ki = 24 nM
8 Ki = 34.3 nM
Protein ID: PT02227, 5-hydroxytryptamine receptor 3A
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000006 HEK293 Homo sapiens (Human)  1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Protein ID: PT00941, 5-hydroxytryptamine receptor 7
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000006 HEK293 Homo sapiens (Human)  1
1
Ki = 840 nM
   TI
   LI
   LO
   TS
Protein ID: PT01005, D(2) dopamine receptor
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000011 CHO Cricetulus griseus (Chinese hamster)  1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CL000873 HEK-GIRK-M4 Homo sapiens (Human)  1
1
Ki = 484 nM
   TI
   LI
   LO
   TS
Biochemical Assays
1 Ki = 13 nM
2 Ki = 90 nM
3 Ki = 1000 nM
Protein ID: PT05367, Multidrug and toxin extrusion protein 1
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000006 HEK293 Homo sapiens (Human)  1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
Protein ID: PT05330, Multidrug and toxin extrusion protein 2
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000006 HEK293 Homo sapiens (Human)  1
1
IC50 = 46000 nM
   TI
   LI
   LO
   TS
Protein ID: PT04591, Solute carrier family 22 member 2
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000006 HEK293 Homo sapiens (Human)  1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Compound
Drug 1 ( Buspirone )
Drug Name Buspirone
Company Bristol-Myers Squibb
Indication
Anxiety disorder
Approved
Target(s)
5-HT 1A receptor (HTR1A)
Agonist