General
Preferred name
SB-271046
Synonyms
SB 271046 hydrochloride ()
SB 271046 (Hydrochloride) ()
SB 271046A ()
SB271046 ()
5-chloro-N-[4-methoxy-3-(piperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide ()
SB-271046 (hydrochloride) ()
SB 271046 ()
SB-271046A ()
P&D ID
PD010546
CAS
209481-24-3
209481-20-9
Tags
available
drug candidate
Drug indication
Discovery agent
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 ¦ÌM)[1].
DESCRIPTION
Potent and selective PAR2 agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective, orally active 5-HT6 antagonist
(Tocriscreen Plus)
DESCRIPTION
SB-271046 is found to be a competitive antagonist with a pA2 of 8.7 in the functional adenylyl cyclase assay which is in good agreement with its binding affinity.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Displacement of [3H]LSD from human recombinant 5HT6 receptor
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
18
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
451.08
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
4.08
TPSA
70.67
Fraction CSP3
0.3
Chiral centers
0.0
Largest ring
6.0
QED
0.61
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Primary Target
5-HT6 Receptors
MOA
Antagonist
serotonin receptor antagonist
Target
HTR6
5-HT6 antagonist
5-HT Receptor
Pathway
GPCR/G protein
Neuronal Signaling
Solubility
Soluble in DMSO (100 mM), and ethanol (50 mM)
Recommended Cell Concentration
100 nM
Source data
