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Found 3468 Enz. Inhib. hit(s) with Target = 'Histamine H1 receptor'
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM81541(CAS_195530 | NSC_195530 | S-Beta-Dimethylhistamine...)
Affinity DataKi:  0.0300nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50017721(1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)pipe...)
Affinity DataKi:  0.0600nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM82479(CAS_132539-06-1 | NSC_4585 | OLANZAPINE | USRE4934...)
Affinity DataKi:  0.0870nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50017721(1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)pipe...)
Affinity DataKi:  0.100nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418268(CHEMBL1767137)
Affinity DataKi:  0.100nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50002099(CHEMBL366965 | Dimethyl-[3-(2-methyl-6H-dibenzo[b,...)
Affinity DataKi:  0.130nMAssay Description:Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50002087(4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thi...)
Affinity DataKi:  0.158nMAssay Description:Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418267(CHEMBL1767138)
Affinity DataKi:  0.158nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391708(CHEMBL1767136)
Affinity DataKi:  0.158nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM84994(CAS_163091 | NSC_163091 | ORG-5222)
Affinity DataKi:  0.160nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

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
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391708(CHEMBL1767136)
Affinity DataKi:  0.162nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.170nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50020712(10,11-dihydro-5-(gamma-dimethylaminopropylidene)-5...)
Affinity DataKi:  0.170nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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))
UniversitÉ

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 H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22872(1-(3-chloro-5,6-dihydrobenzo[b][1]benzothiepin-5-y...)
Affinity DataKi:  0.190nMAssay Description:Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418266(CHEMBL1767141)
Affinity DataKi:  0.200nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22869(6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatric...)
Affinity DataKi:  0.230nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391698(CHEMBL2146801)
Affinity DataKi:  0.251nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418298(CHEMBL1767134)
Affinity DataKi:  0.251nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418265(CHEMBL1767149)
Affinity DataKi:  0.251nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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))
Queen'S Medical Centre

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
TargetHistamine H1 receptor(RAT)
Universit£

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataKi:  0.300nMAssay Description:Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50315206((R)-2-(6-fluoro-3-(1-(thiazol-2-yl)ethyl)-1H-inden...)
Affinity DataKi:  0.300nMAssay Description:Binding affinity at histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50292411((E)-2-(3-(pyrrolidin-1-yl)-1-p-tolylprop-1-enyl)py...)
Affinity DataKi:  0.310nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50002087(4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thi...)
Affinity DataKi:  0.310nMAssay Description:The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418297(CHEMBL1767154)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391702(CHEMBL2146809)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50402823(CHEMBL2208424)
Affinity DataKi:  0.316nMAssay Description:Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50418296(CHEMBL1767140)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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 H1 receptor(RAT)
Universit£

Curated by ChEMBL
LigandPNGBDBM50115644((+/-)-12-Methyl-1,2,3,4,9,13b-hexahydro-2,4a,5-tri...)
Affinity DataKi:  0.320nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391707(CHEMBL2146805)
Affinity DataKi:  0.347nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391699(CHEMBL2146484)
Affinity DataKi:  0.355nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM35256((S)-mianserin | Lerivon | MIANSERIN | MIANSERIN (+...)
Affinity DataKi:  0.360nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50391697(CHEMBL2146806)
Affinity DataKi:  0.398nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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 H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50297307(CHEMBL564226 | R-dimethindene)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

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
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50162956(CHEMBL371352 | Dimethyl-(11-methyl-3,3a,8,12b-tetr...)
Affinity DataKi:  0.430nMAssay Description:Inhibition of [3H]-pyrilamine binding to human Histamine H1 receptor More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50297307(CHEMBL564226 | R-dimethindene)
Affinity DataKi:  0.437nMAssay Description:Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM35938(1-(p-chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpro...)
Affinity DataKi:  0.440nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM50002083(2-[11-(3-Dimethylamino-propylidene)-6,11-dihydro-d...)
Affinity DataKi:  0.480nMAssay Description:Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50079527((3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimet...)
Affinity DataKi:  0.490nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM50316938(1-(4-fluorobenzyl)-2-(1-methylpiperidin-3-yl)-1H-b...)
Affinity DataKi:  0.5nMAssay Description:Antagonist activity at histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Queen'S Medical Centre

Curated by PDSP Ki Database
LigandPNGBDBM22904((2R)-1-(1H-imidazol-5-yl)propan-2-amine | (R)-alph...)
Affinity DataKi:  0.5nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
UniversitÉ

Curated by PDSP Ki Database
LigandPNGBDBM582575(WO2023288027, Cmpd 2f(2S,4R))
Affinity DataKi:  0.5nMAssay Description:The affinity of ligands was determined via radioligand binding techniques using human recombinant receptors expressed in mammalian clonal cells. Deta...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
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