Compounds > ngb 2904
Page last updated: 2024-08-02 11:21:18

ngb 2904

Description

NGB 2904: a dopamine D3 receptor antagonist; structure in first source [MeSH]

N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-9H-fluorene-2-carboxamide : no description available [CHeBI]

Cross-References

ID SourceID
PubMed CID9891901
CHEMBL ID300780
SCHEMBL ID7762650
CHEBI ID92089
MeSH IDM0300148

Synonyms (25)

Synonym
BRD-K05181084-003-02-9
NCGC00167804-01
L016292
CHEMBL300780 ,
n-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]-9h-fluorene-2-carboxamide
9h-fluorene-2-carboxylic acid {4-[4-(2,3-dichloro-phenyl)-piperazin-1-yl]-butyl}-amide
n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9h-fluorene-2-carboxamide
bdbm50071959
ngb-2904
ngb 2904
n-(4-(4-(2,3-dichlorophenyl)-1-piperazinyl)butyl)-3-fluorenylcarboxamide
9h-fluorene-2-carboxamide, n-(4-(4-(2,3-dichlorophenyl)-1-piperazinyl)butyl)-
189060-98-8
n-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-9h-fluorene-2-carboxamide hydrochloride
gtpl6674
SCHEMBL7762650
CHEBI:92089
n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9hfluorene-2-carboxamide
Q27087915
F81743
MS-29174
9h-fluorene-2-carboxamide, n-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-
CS-0012274
HY-12697
AKOS040749022

Drug Classes (1)

ClassDescription
fluorenesAn ortho-fused polycyclic arene in which the skeleton is composed of two benzene rings ortho-fused to cyclopentane.

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency2.2387AID2546

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Integrin beta-3Homo sapiens (human)IC500.0050AID248745
Integrin alpha-IIbHomo sapiens (human)IC500.0050AID248745
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki2.0400AID297339
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.2230AID5254
D(2) dopamine receptorHomo sapiens (human)IC501.2800AID248805; AID297335
D(2) dopamine receptorHomo sapiens (human)Ki0.1912AID1232327; AID238642; AID238970; AID238971; AID297330; AID597451; AID62008; AID749540
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.2230AID5254
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.6420AID37464
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.0012AID238906; AID65603; AID65612
D(1A) dopamine receptorHomo sapiens (human)Ki10.0000AID63349
D(4) dopamine receptorHomo sapiens (human)Ki4.5567AID1232329; AID238949; AID63541
D(1B) dopamine receptorHomo sapiens (human)Ki10.0000AID64186
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.6420AID37464
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.6790AID297340
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.4110AID297341
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.2230AID5254
D(3) dopamine receptorHomo sapiens (human)IC500.0113AID248745; AID248806; AID297336
D(3) dopamine receptorHomo sapiens (human)Ki0.0017AID1232328; AID238643; AID238947; AID238948; AID256758; AID297331; AID597447; AID65129; AID749539
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.6420AID37464
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.5640AID238921; AID65085; AID65246

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
D(3) dopamine receptorHomo sapiens (human)Kd0.0020AID256759

Bioassays (68)

Assay IDTitleYearJournalArticle
AID238970Inhibition of [3H]YM-09151-2 binding to human Dopamine D2L receptor expressed in CHO cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID248805Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D2 receptor2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID62008Compound was evaluated for binding affinity against Dopamine receptor D2 subtype from primate1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID749538Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3391		Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.
AID248745Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID297343Selectivity for human dopamine D3 receptor over human 5HT2A receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID64186Compound was evaluated for binding affinity against human Dopamine receptor D5 transfected in CHO cell membranes1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID238921Inhibition of [125I]IABN binding to rat Dopamine D2L receptor expressed in HEK 293 cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID243003Ratio of binding affinity at dopamine D2L over D3 receptors2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID1232330Selectivity index, ratio of Ki for human dopamine D2 receptor to KI for human dopamine D3 receptor2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
ISSN: 1520-4804		Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID246572Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
AID297333Selectivity for human dopamine D3 receptor over human dopamine D2 receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID243111Relative binding affinity for human dopamine D2 and D3 receptors2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
AID63541Compound was evaluated for binding affinity against human Dopamine receptor D4 transfected in CHO cell membranes1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID238906Inhibition of [125I]IABN binding to rat Dopamine D3 receptor expressed in HEK 293 cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID238947Inhibition of [3H]YM-09151-2 binding to human Dopamine D3 receptor expressed in CHO cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID256759Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
ISSN: 0022-2623		First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
AID249434Relative inhibition of quinpirole stimulation at human dopamine D2 and D3 receptor expressed in CHO cells2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
AID21869Calculated partition coefficient (clogD)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
ISSN: 0960-894X		N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.
AID63638Ratio of binding affinities of D2 receptor to D3 receptor2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
ISSN: 0960-894X		N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.
AID65603Binding affinity at dopamine receptor D3 on Sf9 cells by [125I]IABN displacement.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
ISSN: 0960-894X		Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
AID297340Binding affinity to human 5HT2A receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID63349Compound was evaluated for binding affinity against Dopamine receptor D1 transfected in CHO cell membranes1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID45592Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID749537Selectivity ratio of Ki for human dopamine D2L receptor to Ki for human dopamine D3 receptor2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3391		Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.
AID297336Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID246573Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
AID688180Selectivity ratio of dopamine D1 like receptor to dopamine D3 receptor2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
ISSN: 1464-3405		High-affinity and selective dopamine D₃ receptor full agonists.
AID239022Inhibition of [3H]YM-09151-2 binding to primate Dopamine D2L receptor expressed in CHO cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID256758Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
ISSN: 0022-2623		First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
AID1232331Selectivity index, ratio of Ki for human dopamine D4 receptor to KI for human dopamine D3 receptor2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
ISSN: 1520-4804		Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID238948Inhibition of [125I]IABN binding to human Dopamine D3 receptor expressed in HEK 293 cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID239001Inhibition of [3H]YM-09151-2 binding to primate Dopamine D3 receptor expressed in CHO cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID249049Compound tested for locomotor activity in male Swiss-Webster mice (n=8)2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID597447Displacement of [125I]-IABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
ISSN: 1520-4804		N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID248806Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID297342Selectivity for human dopamine D3 receptor over human 5HT1A receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID229809Relative binding to Dopamine D2 long and D3 receptors (Ratio of Ki)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
ISSN: 0960-894X		Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
AID249398Dopamine receptor D2/D3 selectivity ratio from in vitro functional assays2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID65129Compound was evaluated for binding affinity against human Dopamine receptor D3 transfected in CHO cell membranes to stimulate [3H]thymidine uptake1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID238949Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID1232329Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
ISSN: 1520-4804		Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID297331Displacement of [125I]IABN from human dopamine D3 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID5254Compound was evaluated for binding affinity against 5-hydroxytryptamine 2 receptor from rat1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID749539Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3391		Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.
AID37464Compound was evaluated for binding affinity against Alpha-1 adrenergic receptor from rat1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
ISSN: 0960-894X		NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.
AID65612Binding affinity towards rat Dopamine receptor D3 in Sf9 cells expressing in recombinant baculovirus (Bv) using [125I]IABN as radioligand2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
ISSN: 0960-894X		N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.
AID297344Selectivity for human dopamine D3 receptor over human 5HT2C receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID297335Antagonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID297332Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID65085Binding affinity at dopamine receptor D2 on Sf9 cells by [125I]IABN displacement.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
ISSN: 0960-894X		Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
AID65246Binding affinity towards rat Dopamine receptor D2 in Sf9 cells expressing in recombinant baculovirus (Bv) using [125I]IABN as radioligand2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
ISSN: 0960-894X		N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.
AID297341Binding affinity to human 5HT2C receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID238971Inhibition of [125I]IABN binding to human Dopamine D2L receptor expressed in HEK 293 cells2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID1232328Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
ISSN: 1520-4804		Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID297339Binding affinity to human 5HT1A receptor2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID297330Displacement of [125I]IABN from human dopamine D2 receptor expressed in HEK293 cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
ISSN: 0022-2623		Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
AID749540Displacement of [125I]ABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3391		Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.
AID688179Selectivity ratio of dopamine D2 receptor to dopamine D3 receptor2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
ISSN: 1464-3405		High-affinity and selective dopamine D₃ receptor full agonists.
AID238643Binding affinity for human dopamine D3 receptor2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
AID597451Displacement of [125I]-IABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
ISSN: 1520-4804		N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID237455cLogD was determined2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
ISSN: 0022-2623		Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
AID1232327Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
ISSN: 1520-4804		Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID597448Selectivity ratio Ki for human dopamine D2L receptor to Ki for human dopamine D3 receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
ISSN: 1520-4804		N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
AID238642Binding affinity for human dopamine D2 receptor2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
ISSN: 0022-2623		Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
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
ISSN: 2211-1247		A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1345833Human D3 receptor (Dopamine receptors)2007CNS drug reviews, Summer, Volume: 13, Issue:2
ISSN: 1080-563X		Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction.

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.94)18.2507
2000's16 (47.06)29.6817
2010's14 (41.18)24.3611
2020's3 (8.82)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (94.12%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
N-fluorenylacetamide
0
fluorenes00low000000
4-acetylaminofluorene
0
acetamides;
fluorenes		mitogen00low000000
indecainide
0
fluorenes00low000000
2-hydroxyfluorene
0
fluorenes00low000000
9,9-bis(4-hydroxyphenyl)fluorene
0
fluorenes;
polyphenol		anti-estrogen00low000000
N-(4-methoxyphenyl)carbamic acid (9-fluorenylideneamino) ester
0
fluorenes00low000000
2-(dimethylsulfamoylamino)-9H-fluorene
0
fluorenes00low000000
9-oxo-3-fluorenecarboxylic acid (phenylmethyl) ester
0
fluorenes00low000000
2-{[(9H-9-fluorenylmethoxy)carbonyl]amino}benzoic acid
0
fluorenes00low000000
N2,N7-bis(2,5-dimethylphenyl)-9H-fluorene-2,7-disulfonamide
0
fluorenes00low000000
2-[[5-(3-aminophenyl)-4-methyl-1,2,4-triazol-3-yl]thio]-1-(9H-fluoren-2-yl)ethanone
0
fluorenes00low000000
2-[[(4-ethoxyphenyl)-oxomethyl]amino]acetic acid [2-(9H-fluoren-3-yl)-2-oxoethyl] ester
0
fluorenes00low000000
2-bromo-N-(9-fluorenylideneamino)benzamide
0
fluorenes00low000000
2-butoxy-7-hydroxy-9-fluorenone
0
fluorenes00low000000
4-(9H-fluoren-9-yl)-N-phenyl-1-piperazinecarboxamide
0
fluorenes00low000000
N-(3-chlorophenyl)-4-(9H-fluoren-9-yl)-1-piperazinecarboxamide
0
fluorenes00low000000
9-hydroxyiminofluorene-2,7-disulfonamide
0
fluorenes00low000000
2-[4-(9H-fluoren-9-yl)-1-piperazinyl]-N-(4-methoxyphenyl)acetamide
0
fluorenes00low000000
lumefantrine
0
fluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine		antimalarial00low000000
bms201038
0
(trifluoromethyl)benzenes;
benzamides;
fluorenes;
piperidines		anticholesteremic drug;
MTP inhibitor		00low000000
ledipasvir
0
azaspiro compound;
benzimidazole;
bridged compound;
carbamate ester;
carboxamide;
fluorenes;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organofluorine compound		antiviral drug;
hepatitis C protease inhibitor		00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
haloperidol
2
aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist		1998200522.5low001100
procaine
1
benzoate ester;
substituted aniline;
tertiary amino compound		central nervous system depressant;
drug allergen;
local anaesthetic;
peripheral nervous system drug		201520159.0low000010
sulpiride
1
benzamides;
N-alkylpyrrolidine;
sulfonamide		antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist		2011201113.0low000010
buspirone hydrochloride
1
hydrochlorideanxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist		201520159.0low000010
quinpirole
1
pyrazoloquinolinedopamine agonist2005200519.0low000100
aripiprazole
1
aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist		201520159.0low000010
pramipexole
1
benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger		2012201212.0low000010
bp 897
3
naphthalenecarboxamide2005201117.0low000210
nafadotride
1
aromatic ether;
naphthalenecarboxamide;
nitrile;
pyrrolidines;
tertiary amino compound		dopaminergic antagonist1998199826.0low001000
hymecromone
1
hydroxycoumarinantineoplastic agent;
hyaluronic acid synthesis inhibitor		201520159.0low000010
sb 277011
2
2005201215.5low000110
n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide
4
2003200719.0high000400
s 33084
1
2005200519.0low000100
fauc 346
1
2013201311.0medium000010
fauc 365
4
2004201317.2high000310
pg 01037
6
2005201514.8high000330
gsk598809
1
201520159.0high000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
7-hydroxy-2-n,n-dipropylaminotetralin
1
tetralins201520159.0low000010
sk&f-38393
1
benzazepine;
catechols;
secondary amino compound		2006200618.0low000100
haloperidol
3
aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist		2007201512.7low000120
mitoxantrone
1
dihydroxyanthraquinoneanalgesic;
antineoplastic agent		201720177.0low000010
propranolol
1
naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic		202320231.0low000001
3,4,4a,10b-tetrahydro-4-propyl-2h,5h-(1)benzopyrano(4,3-b)-1,4-oxazin-9-ol
2
2006201513.5low000110
sulpiride
1
benzamides;
N-alkylpyrrolidine;
sulfonamide		antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist		201920195.0low000010
dextroamphetamine
1
1-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent		2007200717.0low000100
sucrose
1
glycosyl glycosidealgal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
sweetening agent		2012201212.0low000010
phencyclidine
1
benzenes;
piperidines		anaesthetic;
neurotoxin;
NMDA receptor antagonist;
psychotropic drug		201520159.0low000010
benzoxazoles
1
1,3-benzoxazoles;
mancude organic heterobicyclic parent		2012201212.0low000010
methamphetamine
1
amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic		2008200816.0low000100
quinpirole
3
pyrazoloquinolinedopamine agonist2007201214.0low000120
spiramide
1
aromatic ether;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		dopaminergic antagonist;
serotonergic antagonist		201920195.0low000010
4-phenylpiperidine
1
2011201113.0low000010
pramipexole
1
benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger		201820186.0low000010
blonanserin
1
organic molecular entity201520159.0low000010
ym 09151-2
1
N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide201920195.0low000010
cholic acid
1
12alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite		201920195.0low000010
cocaine
6
benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic		2005201614.5low000330
raclopride
1
salicylamides2009200915.0low000100
sch 23390
1
benzazepine2009200915.0low000100
bp 897
4
naphthalenecarboxamide2005201515.2low000310
nafadotride
1
aromatic ether;
naphthalenecarboxamide;
nitrile;
pyrrolidines;
tertiary amino compound		dopaminergic antagonist2012201212.0low000010
gr 103691
1
aromatic ketone201920195.0low000010
sb 277011
5
2005201714.0medium000320
heroin
1
morphinane alkaloidmu-opioid receptor agonist;
opioid analgesic;
prodrug		2009200915.0low000100
n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide
1
2010201014.0medium000100
n-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide
1
201520159.0low000010
fmrfamide
1
201920195.0low000010
neuropeptide y
1
201920195.0low000010
piperidines
2
2011201511.0low000020
yqa14
1
2012201212.0medium000010
peptide yy
1
201920195.0low000010
guanosine 5'-o-(3-thiotriphosphate)
1
nucleoside triphosphate analogue2012201212.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Anochlesia0
1
2012201212.0low000010
Cancer of Colon0
1
201720177.0low000010
Cancer of Lung0
1
201720177.0low000010
Carcinoma, Non-Small Cell Lung0
1
201720177.0low000010
Carcinoma, Non-Small-Cell Lung0
1
201720177.0low000010
Chemical Dependence0
5
2005201515.2medium000410
Cocaine Abuse0
4
2005201614.2medium000220
Cocaine-Related Disorders0
4
2005201614.2medium000220
Colonic Neoplasms0
1
201720177.0low000010
Congenital Zika Syndrome0
1
202020204.0low000010
Depression0
1
201820186.0low000010
Disease Models, Animal0
6
2007202010.5medium000240
Lung Neoplasms0
1
201720177.0low000010
Obesity0
1
2008200816.0low000100
Recrudescence0
1
2005200519.0low000100
Substance-Related Disorders0
5
2005201515.2medium000410
Zika Virus Infection0
1
202020204.0low000010

Pharmacokinetics (1)

ArticleYear
Characterization of the transport, metabolism, and pharmacokinetics of the dopamine D3 receptor-selective fluorenyl- and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse.
The Journal of pharmacology and experimental therapeutics, , Volume: 333, Issue:3		2010

Bioavailability (1)

ArticleYear
Characterization of the transport, metabolism, and pharmacokinetics of the dopamine D3 receptor-selective fluorenyl- and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse.
The Journal of pharmacology and experimental therapeutics, , Volume: 333, Issue:3		2010

Dosage (1)

ArticleYear
Effects of two novel D3-selective compounds, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the reinforcing and discrimin
The Journal of pharmacology and experimental therapeutics, , Volume: 321, Issue:2		2007