Page last updated: 2024-12-11

sb 215505

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

SB 215505: a neuroleptic with equivalent or higher antagonist affinity for 5-HT2 than for dopamine D2 receptor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6603999
CHEMBL ID525998
MeSH IDM0304681
PubMed CID10449757
CHEMBL ID2110371
SCHEMBL ID1157493
MeSH IDM0304681

Synonyms (44)

Synonym
EU-0100821
sb-215505, solid, >98% (hplc)
NCGC00015926-01
lopac-s-1068
NCGC00094152-01
NCGC00094152-02
L023993
NCGC00015926-02
NCGC00015926-04
CHEMBL525998
6-chloro-5-methyl-n-quinolin-4-yl-2,3-dihydroindole-1-carboxamide
HMS3262F03
sb215505
CCG-204905
NCGC00015926-03
6-chloro-5-methyl-1-5-quinolycarbamoyl-indoline
LP00821
NCGC00261506-01
tox21_500821
DTXSID70424971
J-009894
sr-01000076012
SR-01000076012-1
Q7388906
SDCCGSBI-0050798.P002
gtpl190
sb-215505
6-chloro-5-methyl-n-quinolin-5-yl-2,3-dihydroindole-1-carboxamide
sb 215505
L018293
6-chloro-5-methyl-1-(5-quinolylcarbamoyl)indoline
bdbm85859
162100-15-4
CHEMBL2110371
SCHEMBL1157493
6-chloro-2,3-dihydro-5-methyl-n-5-quinolinyl-1h-indole-1-carboxamide
AKOS025293478
CS-0011469
HY-18596
6-chloro-5-methyl-n-(5-quinolinyl)-2,3-dihydro-1h-indole-1-carboxamide
6-chloro-5-methyl-n-(quinolin-5-yl)indoline-1-carboxamide
Q27088701
SB73117
AS-84171

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonism of the 5-HT(2B) receptor, (b) low impact of serum proteins on potency, and (c) desirable pharmacokinetic properties."( A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Choi, Y; Cogan, D; Flegg, A; Kahrs, A; Loke, P; Meyn, O; Moss, N; Nagaraja, R; Napier, S; Parker, A; Ramsden, P; Sarko, C; Skow, D; Thomas Peterson, J; Tomlinson, J; Tye, H; Whitaker, M, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (37)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency0.05800.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency21.19230.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency0.02510.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency7.07950.35487.935539.8107AID624146
Microtubule-associated protein tauHomo sapiens (human)Potency12.58930.180013.557439.8107AID1460
arylsulfatase AHomo sapiens (human)Potency6.01201.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency40.34590.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency22.38720.540617.639296.1227AID2364; AID2528
hexokinase-4 isoform 1Homo sapiens (human)Potency3.98112.511913.800328.1838AID743205
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency8.492123.934123.934123.9341AID1967
D(1A) dopamine receptorHomo sapiens (human)Potency1.15810.02245.944922.3872AID488982
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.23410.354828.065989.1251AID504847
glucokinase regulatory proteinHomo sapiens (human)Potency3.98112.511913.800328.1838AID743205
flap endonuclease 1Homo sapiens (human)Potency4.74440.133725.412989.1251AID588795
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency1.99530.050127.073689.1251AID588590
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.94330.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency79.43280.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency0.00090.891312.067628.1838AID1487
chaperonin GroELMethanococcus maripaludis S2Potency50.118731.622831.622831.6228AID488978
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency1.69440.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.03850.00011.18738.9125AID351748; AID351749
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1413513Ratio of IC50 for antagonist activity at recombinant human 5-HT2B receptor in presence of human serum albumin to IC50 for antagonist activity at recombinant human 5-HT2B receptor in absence of human serum albumin2018MedChemComm, Jun-01, Volume: 9, Issue:6
Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists.
AID351748Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
AID351744Selectivity for 5-HT2B receptor over 5-HT2A receptor2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
AID351753Selectivity for 5-HT2B receptor over 5-HT2C receptor2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
AID351749Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A1999British journal of pharmacology, Feb, Volume: 126, Issue:3
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.35)18.2507
2000's10 (43.48)29.6817
2010's7 (30.43)24.3611
2020's5 (21.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.54

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.54 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]