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Found 903 with Last Name = 'de graaf' and Initial = 'c'
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354647(CHEMBL1834244)
Affinity DataKi:  0.0250nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354644(CHEMBL1834218)
Affinity DataKi:  0.0250nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354650(CHEMBL1834247)
Affinity DataKi:  0.0470nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor 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
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM104692(US8569311, E-5)
Affinity DataKi:  0.200nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More 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
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354649(CHEMBL1834246)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354651(CHEMBL1834248)
Affinity DataKi:  0.330nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM50318701(CHEMBL1083659 | MK-4305 | [(7R)-4-(5-Chloro-1,3-be...)
Affinity DataKi:  0.398nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
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))
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
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354645(CHEMBL1834219)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]DAMGO from rat brain Mu-type opioid receptor 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
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
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM50093793(E-2006 | Lemborexant)
Affinity DataKi:  0.501nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
TargetC-X-C chemokine receptor type 4(Homo sapiens (Human))TBA
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM154947(US9000029, 26)
Affinity DataKi:  0.631nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM104692(US8569311, E-5)
Affinity DataKi:  0.631nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
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

Curated by ChEMBL
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM50318701(CHEMBL1083659 | MK-4305 | [(7R)-4-(5-Chloro-1,3-be...)
Affinity DataKi:  0.794nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
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 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(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
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

Curated by ChEMBL
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
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM334973(US11040966, Example 5.36 | US9732075, Example 5.36...)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
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 H4 receptor(Homo sapiens (Human))
Vu University 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 H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
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
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM334973(US11040966, Example 5.36 | US9732075, Example 5.36...)
Affinity DataKi:  1.60nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More 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

TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
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
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354644(CHEMBL1834218)
Affinity DataKi:  1.70nMAssay Description:Displacement of [3H]Ile-deltorphin-2 from rat brain delta-type opioid receptor 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
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 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
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM50520181(CHEMBL2413522)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
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
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
Vrije Universiteit Brussel

Curated by ChEMBL
LigandPNGBDBM50354650(CHEMBL1834247)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]Ile-deltorphin-2 from rat brain delta-type opioid receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Sosei Heptares

Curated by ChEMBL
LigandPNGBDBM50093793(E-2006 | Lemborexant)
Affinity DataKi:  2.5nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
TargetHistamine H1 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50202830(CHEMBL3905009)
Affinity DataKi:  2.5nMAssay 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
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
TargetHistamine H3 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22541(Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H...)
Affinity DataKi:  2.82nMAssay 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
LigandPNGBDBM50516709(CHEMBL4588726)
Affinity DataKi:  3.20nMAssay 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
LigandPNGBDBM50202726(CHEMBL3955589)
Affinity DataKi:  3.20nMAssay 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 H4 receptor(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM50491206(CHEMBL2375772)
Affinity DataKi:  3.20nMAssay Description:Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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