Compile Data Set for Download or QSAR
Report error Found 15189 Enz. Inhib. hit(s) with Target = 'Kappa-type opioid receptor'
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50035476(N-[(S)-1-(3-Amino-phenyl)-2-pyrrolidin-1-yl-ethyl]...)
Affinity DataIC50: 0.000320nMAssay Description:Binding affinity kappa opioid receptor in guinea pig brain membranes; using 1 nM [3H]U-69593 as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM224024(Dynorphin A (1-13) | YGGFLRRXRPKLK | BDBM50241435)
Affinity DataKi:  0.000800nMAssay Description:Binding affinity towards Wild-type kappa opioid receptor expressed in HEK cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50561762(CHEMBL4785966)
Affinity DataEC50:  0.00100nMAssay Description:Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50561764(CHEMBL4743180)
Affinity DataEC50:  0.00100nMAssay Description:Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM602186(US11643436, Compound TM-9A)
Affinity DataEC50:  0.00100nMAssay Description:Forskolin can stimulate the release of cAMP from HEK293 cells with high expression of human κ (or μ, or δ)-opioid receptors. The κ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2023
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235813(US9359399, 27)
Affinity DataEC50: <0.00100nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235811(US9359399, 25)
Affinity DataEC50:  0.00270nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM393487(US9963460, 13)
Affinity DataEC50:  0.00280nMAssay Description:In a [3SS] GTPγS binding test, the opioid receptor agonist activity of test compounds based on a GTP-GDP exchange reaction was evaluated. In the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2020
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50561760(CHEMBL4791124)
Affinity DataEC50:  0.00300nMAssay Description:Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235785(US9359399, 2 | CVD-0019439)
Affinity DataEC50:  0.00300nMAssay Description:Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50195673(N-cyclopropylmethyl-14beta-[3'-(4'-chlorophenyl)pr...)
Affinity DataIC50: 0.00300nMAssay Description:Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/8/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50366764(MCL-117 | CHEMBL1790045)
Affinity DataKi:  0.00300nMAssay Description:Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50366764(MCL-117 | CHEMBL1790045)
Affinity DataKi:  0.00300nMAssay Description:Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/4/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50002186(CHEMBL440987 | Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Lys...)
Affinity DataKi:  0.00420nMAssay Description:Inhibition of [3H]- bremazocine to opioid receptor kappa of guinea pig cerebral membranes was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235815(US9359399, 31)
Affinity DataEC50:  0.00420nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50269287(CHEMBL4087151)
Affinity DataEC50:  0.00466nMAssay Description:Agonist activity at human kappa opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235816(US9359399, 32)
Affinity DataEC50:  0.00500nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50378578(CHEMBL1627119)
Affinity DataKi:  0.00500nMAssay Description:Antagonist activity at kappa opioid receptor expressed in HEK293 cells assessed as inhibition of compound 16-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235792(US9359399, 36)
Affinity DataEC50:  0.00520nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Mouse)
Cara Therapeutics

US Patent
LigandPNGBDBM235813(US9359399, 27)
Affinity DataEC50:  0.00560nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50195666(N-cyclopropylmethyl-14beta-[3'-(4'-chlorophenyl)pr...)
Affinity DataIC50: 0.00600nMAssay Description:Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/8/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50626414(CHEMBL5431513)
Affinity DataKi:  0.00600nMAssay Description:Binding affinity to wild type human KOR assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50102711(7-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carbox...)
Affinity DataKi:  0.00600nMAssay Description:Antagonist activity on agonist (U50,488) stimulated [35S]GTP-gamma-S, binding in cloned opioid receptor kappa 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430586(CHEMBL2338721)
Affinity DataEC50:  0.00610nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235818(US9359399, 35)
Affinity DataEC50:  0.00640nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50002182(CHEMBL415617 | Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Lys...)
Affinity DataKi:  0.00670nMAssay Description:Inhibition of [3H]- bremazocine to opioid receptor kappa of guinea pig cerebral membranes was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430613(CHEMBL2338723)
Affinity DataEC50:  0.00700nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430612(CHEMBL2338724)
Affinity DataEC50:  0.00770nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM602189(US11643436, Compound TM-26)
Affinity DataEC50:  0.00800nMAssay Description:Forskolin can stimulate the release of cAMP from HEK293 cells with high expression of human κ (or μ, or δ)-opioid receptors. The κ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2023
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50274347((2E)-N-[(5R,6R)-17-(cyclopropylmethyl)-4,5-epoxy-3...)
Affinity DataEC50:  0.00820nMAssay Description:Agonist activity at kappa opioid receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235789(US9359399, 28)
Affinity DataEC50:  0.00830nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235812(US9359399, 26)
Affinity DataEC50:  0.00830nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM602188(US11643436, Compound TM-22B)
Affinity DataEC50:  0.00900nMAssay Description:Forskolin can stimulate the release of cAMP from HEK293 cells with high expression of human κ (or μ, or δ)-opioid receptors. The κ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2023
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM602184(US11643436, Compound TM-7)
Affinity DataEC50:  0.00900nMAssay Description:Forskolin can stimulate the release of cAMP from HEK293 cells with high expression of human κ (or μ, or δ)-opioid receptors. The κ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2023
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430611(CHEMBL2338725)
Affinity DataEC50:  0.00980nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50001714(2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-13-ox...)
Affinity DataKi:  0.0100nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/2/2012
Entry Details
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50561763(CHEMBL4756370)
Affinity DataEC50:  0.0100nMAssay Description:Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50242686(CHEMBL4077003)
Affinity DataKi:  0.0100nMAssay Description:Displacement of [3H]DPN from guinea pig kappa opioid receptor expressed in CHOK1 cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2019
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50242686(CHEMBL4077003)
Affinity DataKi:  0.0100nMAssay Description:Displacement of [3H]DPN from guinea pig kappa opioid receptor expressed in CHOK1 cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2019
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Guinea pig)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50229232(CHEMBL610527)
Affinity DataKi:  0.0100nMAssay Description:Compound was evaluated for the binding affinity to opioid receptor kappa using [3H]-EK as radioligand in guinea pig brain membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/21/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50130563((R)-7-hydroxy-N-((S)-1-((3R,4R)-4-(3-hydroxyphenyl...)
Affinity DataKi:  0.0100nMAssay Description:Antagonist activity at kappa opioid receptor (unknown origin) assessed as stimulation of [35S]GTPgammaSMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430622(CHEMBL2338747)
Affinity DataEC50:  0.0110nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235790(US9359399, 30)
Affinity DataEC50:  0.0116nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Mouse)
Cara Therapeutics

US Patent
LigandPNGBDBM235795(US9359399, 7)
Affinity DataEC50:  0.0120nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50430587(CHEMBL2338720)
Affinity DataEC50:  0.0130nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM199410(US9221831, 75)
Affinity DataKi:  0.0140nMpH: 7.4Assay Description:Radioligand dose displacement assays used 0.4 nM [3H]-U69,593 (GE Healthcare, Piscataway, N.J.; 40 Ci/mmole) with 15 μg membrane protein (recomb...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/8/2016
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM235814(US9359399, 29)
Affinity DataEC50:  0.0145nMT: 2°CAssay Description:Mouse R1.G1 cells (ATCC, Manassas, Va.) were grown in suspension in high glucose-DMEM (Dulbecco's Modified Eagle's Medium, Cellgro, Herndon, Va.) con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50598862(CHEMBL5178795)
Affinity DataEC50:  0.0150nMAssay Description:Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50304175(17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-e...)
Affinity DataKi:  0.0150nMAssay Description:Antagonist activity at kappa opioid receptor expressed in HEK293 cells assessed as inhibition of compound 16-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMed
TargetKappa-type opioid receptor(Human)
University of Minnesota

Curated by ChEMBL
LigandPNGBDBM50159165(2S,4aR,6a(R,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(fura...)
Affinity DataEC50:  0.0150nMAssay Description:Agonist activity at human KOR expressed in HEK293T cells assessed as inhibition of Galphai-mediated cAMP accumulation after 15 mins by microbeta coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2021
Entry Details Article
PubMed
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