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Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50397290(CHEMBL475331 | VUF-10147)
Affinity DataKi:  0.0513nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50546794(CHEMBL4777335)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of recombinant human cathepsin S using Z-VVR-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.178nMAssay Description:Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50099623(4-[2-(4,4-Dimethyl-pent-1-ynyl)-cyclopropyl]-1H-im...)
Affinity DataKi:  0.180nMAssay Description:Ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortexMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.251nMAssay Description:Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22541(Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H...)
Affinity DataKi:  0.339nM ΔG°:  -54.1kJ/molepH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50031228(CHEMBL420316)
Affinity DataKi:  0.398nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataKi:  0.398nMAssay Description:Inhibition of full length recombinant human PDE4B1 expressed in Sf21 insect cells using cAMP as substrate by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50099622(1-Cyclohexylmethyl-3-[2-(1H-imidazol-4-yl)-cyclopr...)
Affinity DataKi:  0.400nMAssay Description:Ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortexMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22542(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)
Affinity DataKi:  0.407nM ΔG°:  -53.6kJ/molepH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516710(CHEMBL4469024)
Affinity DataKi:  0.417nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50053631(2-(4-Methyl-piperazin-1-yl)-quinoline | 2-(4-methy...)
Affinity DataKi:  0.457nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50150945(CHEBI:81390 | Immepip)
Affinity DataKi:  0.479nMAssay Description:Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22542(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)
Affinity DataKi:  0.501nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50150945(CHEBI:81390 | Immepip)
Affinity DataKi:  0.501nMAssay Description:Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 4(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50335557(CHEMBL1652605 | N,N-dipropyl-N'-[4-({[(1H-imidazol...)
Affinity DataKi:  0.610nMAssay Description:Binding affinity to CXCR4 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516713(CHEMBL4448535)
Affinity DataKi:  0.631nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50427452(CHEMBL2326941)
Affinity DataKi:  0.631nMAssay Description:Inhibition of full length recombinant human PDE4B1 expressed in Sf21 insect cells using cAMP as substrate by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22916(5-{3-[(4-iodophenyl)methoxy]propyl}-1H-imidazole |...)
Affinity DataKi:  0.631nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516707(CHEMBL4588983)
Affinity DataKi:  0.794nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22548(2-[3-(1H-imidazol-4-ylmethyl)phenyl]-4,4,6-trimeth...)
Affinity DataKi:  1nM ΔG°:  -51.4kJ/mole EC50:  2nMpH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM22564(2-arylbenzimidazole derivative, 10 | 2-{2-chloro-4...)
Affinity DataKi:  1nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516717(CHEMBL4582006)
Affinity DataKi:  1nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Mus musculus)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50514105(CHEMBL4441731)
Affinity DataKi:  1nMAssay Description:Displacement of [3H]NAMH from mouse H3R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50475340(Methimepip)
Affinity DataKi:  1nMAssay Description:Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50419448(CHEMBL1923026)
Affinity DataKi:  1.02nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50419444(CHEMBL43934 | VUF-5228)
Affinity DataKi:  1.05nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50397307(CHEMBL489062 | VUF-10349)
Affinity DataKi:  1.12nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50419456(CHEMBL1923034)
Affinity DataKi:  1.15nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22567(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516716(CHEMBL4474226)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50397291(CHEMBL443764 | VUF-10249)
Affinity DataKi:  1.35nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50474424(CHEMBL153051)
Affinity DataKi:  1.40nMAssay Description:Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50397284(CHEMBL2169970)
Affinity DataKi:  1.45nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM50361015(CHEMBL592379)
Affinity DataKi:  1.55nMAssay Description:Binding affinity to rat histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22911(2-(3H-imidazol-4-yl)ethylsulfanylmethanimidamide |...)
Affinity DataKi:  1.58nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50419048(CHEMBL1824048)
Affinity DataKi:  1.58nMAssay Description:Displacement of [3H]granisetron from human 5-HT3AR expressed in HEK293 cells after 24 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50414391(CHEMBL1202332 | CHEMBL553423)
Affinity DataKi:  1.58nMAssay Description:Agonistic activity at histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM50414391(CHEMBL1202332 | CHEMBL553423)
Affinity DataKi:  1.58nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22911(2-(3H-imidazol-4-yl)ethylsulfanylmethanimidamide |...)
Affinity DataKi:  1.58nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50073179(8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-be...)
Affinity DataKi:  1.60nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50397288(CHEMBL2169966)
Affinity DataKi:  1.62nMAssay Description:Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM50419455(CHEMBL1923033)
Affinity DataKi:  1.62nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50127605((1S,2S)-2-(1H-Imidazol-4-yl)-cyclopropylamine | (1...)
Affinity DataKi:  1.70nMAssay Description:In vitro binding affinity was measured against Histamine H3 receptor on rat cerebral cortex.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516706(CHEMBL4514700)
Affinity DataKi:  1.80nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22538(4-Benzyl-1H-imidazole derivative, 19 | 4-{[3-(2-ph...)
Affinity DataKi:  2nM ΔG°:  -49.7kJ/molepH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50202722(CHEMBL3906929)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22567(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)
Affinity DataKi:  2.09nMAssay Description:Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516708(CHEMBL4581343)
Affinity DataKi:  2.10nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50516719(CHEMBL4554533)
Affinity DataKi:  2.5nMAssay Description:Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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