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Found 179 Enz. Inhib. hit(s) with all data for entry = 50008317
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518036(CHEMBL4467777 | US11484525, Compound BD-122LS-PZM2...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [3H]-Diprenorphine from mu opioid receptor (unknown origin) expressed in sf9 insect cell membranes after 1 hr by liquid scintillation...More data for this Ligand-Target Pair
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518026(CHEMBL4449152)
Affinity DataKi:  42nMAssay Description:Displacement of [3H]-Diprenorphine from mu opioid receptor (unknown origin) expressed in sf9 insect cell membranes after 1 hr by liquid scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518058(CHEMBL4463417)
Affinity DataKi:  2.50E+3nMAssay Description:Displacement of [3H]-Diprenorphine from mu opioid receptor (unknown origin) expressed in sf9 insect cell membranes after 1 hr by liquid scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50061101(4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-...)
Affinity DataIC50:  1.00E+3nMAssay Description:Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionMore data for this Ligand-Target Pair
TargetEndothelin-1 receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50061101(4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-...)
Affinity DataIC50:  1.59E+3nMAssay Description:Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518021(CHEMBL610279)
Affinity DataEC50:  1.10nMAssay Description:Agonist activity at full-length Renilla luciferase 8 fused with c-terminal human kappa opioid receptor expressed in HEK293T cells assessed as inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518022(CHEMBL4458783)
Affinity DataEC50:  31nMAssay Description:Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 1 hrs by TopCou...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518023(CHEMBL4513533 | US10751335, Example 14)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetAdenosine receptor A3(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50389129(CHEMBL2064661)
Affinity DataEC50:  13nMAssay Description:Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM17657((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Affinity DataEC50:  1.60E+4nMAssay Description:Agonist activity at mGlu5 receptor (unknown origin) expressed in CHO cells assessed as increase in Gq-mediated PI hydrolysis after 45 mins by yttrium...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM442801(WAY-308264)
Affinity DataEC50:  1.10nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50130293(7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}...)
Affinity DataEC50:  4nMAssay Description:Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitmentMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetAdenosine receptor A3(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50389151(CHEMBL2064634)
Affinity DataEC50:  316nMAssay Description:Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincuba...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM60917(9-chloranyl-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro...)
Affinity DataEC50:  32nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
TargetCannabinoid receptor 2(MOUSE)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50303526((1-Pentyl-1H-indol-3-yl)(2,2,3,3-tetramethylcyclop...)
Affinity DataEC50:  95nMAssay Description:Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-ar...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetApelin receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518024(CHEMBL4438370)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at GFP10 tagged human APJ receptor expressed in HEK293 cells harboring Rluc2-beta-arrestin1 assessed as increase in beta-arrestin1 r...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50387454(CHEMBL2047474)
Affinity DataEC50:  1.00E+3nMAssay Description:Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by lumine...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCannabinoid receptor 2(MOUSE)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518025(CHEMBL4467282)
Affinity DataEC50:  15nMAssay Description:Inverse agonist activity at mouse CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 5 mins ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHydroxycarboxylic acid receptor 2(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM23515(CHEMBL573 | Niacin | Nicotinic Acid | [5, 6-3H]-ni...)
Affinity DataEC50:  14.5nMAssay Description:Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesMore data for this Ligand-Target Pair
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518026(CHEMBL4449152)
Affinity DataEC50:  180nMAssay Description:Agonist activity at Gi/o coupled human mu opioid receptor expressed in HEK293T cells co-expressing luciferase based cAMP biosensor and GRK2 assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518027(CHEMBL4550815 | US11498896, Compound 1)
Affinity DataEC50:  120nMAssay Description:Agonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518028(CHEMBL4472022)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50004917(3-Allyl-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-be...)
Affinity DataEC50:  2nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50274531(6-Chloro-3-methyl-1-m-tolyl-2,3,4,5-tetrahydro-1H-...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50004918((+/-)-APD3-Allyl-1-phenyl-2,3,4,5-tetrahydro-1H-be...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM442801(WAY-308264)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM86277(MCL-210)
Affinity DataEC50:  0.120nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518028(CHEMBL4472022)
Affinity DataEC50:  0.300nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50004917(3-Allyl-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-be...)
Affinity DataEC50:  0.730nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50274531(6-Chloro-3-methyl-1-m-tolyl-2,3,4,5-tetrahydro-1H-...)
Affinity DataEC50:  0.200nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
TargetD(1A) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM60917(9-chloranyl-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro...)
Affinity DataEC50:  2.80nMAssay Description:Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation aft...More data for this Ligand-Target Pair
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50164848(CHEMBL3798179)
Affinity DataEC50:  154nMAssay Description:Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitmentMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518029(CHEMBL4442260)
Affinity DataEC50:  0.710nMAssay Description:Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment after 20 mins measured for 1 sec by BRE...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518030(CHEMBL4467404)
Affinity DataEC50:  2.90nMAssay Description:Agonist activity at human dopamine D2long receptor (unknown origin) expressed in HEK293T cells co-expressing TEV fused-beta-Arrestin2 and GRK2 assess...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518031(CHEMBL4445841)
Affinity DataEC50:  6.30nMAssay Description:Agonist activity at human dopamine D2long receptor (unknown origin) expressed in HEK293T cells co-expressing TEV fused-beta-Arrestin2 and GRK2 assess...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518030(CHEMBL4467404)
Affinity DataEC50:  23nMAssay Description:Agonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293T cells co-expressing luciferase based cAMP biosensor assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNociceptin receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518032(CHEMBL4456531)
Affinity DataEC50:  72nMAssay Description:Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediatel...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNociceptin receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50255899(1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3S)-3...)
Affinity DataEC50:  1.59E+3nMAssay Description:Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitmentMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50325534(CHEMBL267495 | nalfurafine)
Affinity DataEC50:  5.20nMAssay Description:Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation...More data for this Ligand-Target Pair
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50325534(CHEMBL267495 | nalfurafine)
Affinity DataEC50:  0.5nMAssay Description:Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Wes...More data for this Ligand-Target Pair
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50325534(CHEMBL267495 | nalfurafine)
Affinity DataEC50:  1.40nMAssay Description:Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by ...More data for this Ligand-Target Pair
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50491417(22-THIOCYANATOSALVINORIN A)
Affinity DataEC50:  5.20nMAssay Description:Agonist activity at kappa opioid receptor (unknown origin) expressed in HEK cells co-expressing luciferase based cAMP biosensor assessed as increase ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50008984(4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-ph...)
Affinity DataEC50:  43nMAssay Description:Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayMore data for this Ligand-Target Pair
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518033(CHEMBL4537962)
Affinity DataEC50:  76nMAssay Description:Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 1 hrs by TopCou...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518022(CHEMBL4458783)
Affinity DataEC50:  329nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM21130(N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl...)
Affinity DataEC50:  205nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in bet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM21130(N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl...)
Affinity DataEC50:  131nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in bet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50254705(CHEMBL4068633)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in bet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM65817(2-[5-[(3,4-dichlorobenzyl)thio]-4-(2-furfuryl)-1,2...)
Affinity DataEC50:  870nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in bet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Homo sapiens (Human))
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50518034(CHEMBL4451128)
Affinity DataEC50:  374nMAssay Description:Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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