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Found 2479 with Last Name = 'leurs' and Initial = 'r'
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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527524(CHEMBL4566742)
Affinity DataKi:  0.0617nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.0900nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527552(CHEMBL4435111)
Affinity DataKi:  0.120nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527532(CHEMBL4441748)
Affinity DataKi:  0.123nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527531(CHEMBL4524402)
Affinity DataKi:  0.155nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527537(CHEMBL4453005)
Affinity DataKi:  0.155nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.160nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527528(CHEMBL4441871)
Affinity DataKi:  0.162nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527550(CHEMBL4461456)
Affinity DataKi:  0.170nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM112780(US8629135, SW-07)
Affinity DataKi:  0.178nMAssay Description:Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scin...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527535(CHEMBL4589927)
Affinity DataKi:  0.224nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527533(CHEMBL4592553)
Affinity DataKi:  0.234nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
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 H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.280nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527555(CHEMBL4530777)
Affinity DataKi:  0.302nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527567(CHEMBL4473426)
Affinity DataKi:  0.316nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527560(CHEMBL4444578)
Affinity DataKi:  0.316nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.320nMMore 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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527554(CHEMBL4460623)
Affinity DataKi:  0.355nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527559(CHEMBL4591859)
Affinity DataKi:  0.389nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore 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
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 H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
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
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))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
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

LigandPNGBDBM22542(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)
Affinity DataKi:  0.501nMAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More 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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527525(CHEMBL4522249)
Affinity DataKi:  0.513nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527529(CHEMBL4454600)
Affinity DataKi:  0.562nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM22567(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)
Affinity DataKi:  0.570nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM86032(trans-H2-PAT(-) | trans-PAT)
Affinity DataKi:  0.580nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 7(Rattus norvegicus (rat))
U. 109

Curated by PDSP Ki Database
LigandPNGBDBM10755(14C-5-hydroxy tryptamine creatinine disulfate | 2-...)
Affinity DataKi:  0.600nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22916(5-{3-[(4-iodophenyl)methoxy]propyl}-1H-imidazole |...)
Affinity DataKi:  0.630nMAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527527(CHEMBL4466777)
Affinity DataKi:  0.661nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527534(CHEMBL4472307)
Affinity DataKi:  0.676nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Homo sapiens (Human))
University Of Antwerp

Curated by ChEMBL
LigandPNGBDBM50527530(CHEMBL4461705)
Affinity DataKi:  0.676nMAssay Description:Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit basedMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM35938(1-(p-chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpro...)
Affinity DataKi:  0.690nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM50292411((E)-2-(3-(pyrrolidin-1-yl)-1-p-tolylprop-1-enyl)py...)
Affinity DataKi:  0.690nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
University Of North Carolina At Chapel Hill

Curated by PDSP Ki Database
LigandPNGBDBM22567(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)
Affinity DataKi:  0.740nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

LigandPNGBDBM22910(4-(1H-imidazol-5-ylmethyl)pyridine | Immethridine)
Affinity DataKi:  0.794nMAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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