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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 46 hits in this display   

TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167072(CHEMBL3799125)
Affinity DataKi:  0.0300nMAssay Description:Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167072(CHEMBL3799125)
Affinity DataKi:  0.0340nMAssay Description:Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-1 adrenergic receptor(Mus musculus)
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167072(CHEMBL3799125)
Affinity DataKi:  0.210nMAssay Description:Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-1 adrenergic receptor(Rattus norvegicus (Rat))
RzeszóW University Of Technology

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  0.810nMAssay Description:Displacement of [3H]CGP12177 from beta1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  0.880nMAssay Description:Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  0.880nMAssay Description:Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  1.10nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetBeta-1 adrenergic receptor(Homo sapiens (Human))
UniversitÄT WÜRzburg

Curated by PDSP Ki Database
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  1.70nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Rattus norvegicus (rat))
Rzesz£W University Of Technology

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  2.20nMAssay Description:Displacement of [3H]Prazosin from alpha1 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 1A(Rattus norvegicus (rat))
Universit£

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  3.20nMAssay Description:Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacementMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-1 adrenergic receptor(Mus musculus)
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  3.40nMAssay Description:Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  3.40nMAssay Description:Displacement of [3H]Clonidine from alpha2 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  26nMAssay Description:Displacement of [3H]spiperone from human D2S receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50167072(CHEMBL3799125)
Affinity DataKi:  49nMAssay Description:Displacement of [3H]spiperone from human D2S receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-3 adrenergic receptor(Homo sapiens (Human))
UniversitÄT WÜRzburg

Curated by PDSP Ki Database
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKi:  247nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
University Of Helsinki

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  1.30E+3nMAssay Description:Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
University Of Helsinki

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataKi:  1.40E+3nMAssay Description:Displacement of [125I]-orexin A from human OX2 receptor expressed in CHO cell membranes after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  350nMAssay Description:Inhibitory concentration against IKr potassium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetOrexin receptor type 2(Homo sapiens (Human))
University Of Helsinki

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataIC50:  900nMAssay Description:Displacement of [125I]-orexin A from human OX2 receptor expressed in CHO cell membranes after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1B1(Homo sapiens (Human))
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataIC50:  1.10E+3nMAssay Description:Inhibition of human CYP1B1 using 7-ethyl-O-resorufin as substrate incubated for 30 mins in presence of NADPH by EROD assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium channel subfamily K member 2(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.60E+3nMAssay Description:Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currentsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
University Of Helsinki

Curated by ChEMBL
LigandPNGBDBM50167073(CHEMBL3798017)
Affinity DataIC50:  2.30E+3nMAssay Description:Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 1(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  3.40E+3nMAssay Description:In vitro inhibition of geranylgeranyl-protein transferase type-IMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  4.60E+3nMAssay Description:TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  6.00E+3nMAssay Description:TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  6.60E+3nMAssay Description:TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 2(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  7.50E+3nMAssay Description:Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium channel subfamily K member 10(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  7.60E+3nMAssay Description:Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currentsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.05E+4nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.05E+4nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.05E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetUDP-glucuronosyltransferase 1A1(Homo sapiens (Human))
University Of Minnesota

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.20E+4nMAssay Description:Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  1.26E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetPotassium channel subfamily K member 2(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  2.03E+4nMAssay Description:Inhibition of of human TREK1 expressed in oocytes assessed as reversible current depressionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium channel subfamily K member 10(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  2.40E+4nMAssay Description:Inhibition of of TREK2 (unknown origin) expressed in oocytes assessed as reduction in channel currentsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 1A1(Homo sapiens (Human))
University Of Minnesota

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  2.70E+4nMAssay Description:Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetToll-like receptor 4(Homo sapiens (Human))
School Of Pharmaceutical Sciences

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  3.22E+4nMAssay Description:Antagonist activity at human TLR4 expressed in HEK blue cells coexpressing MD-2/CD14 assessed as inhibition of LPS-induced NF-kappaB activation-media...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMultidrug and toxin extrusion protein 1(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50:  9.24E+4nMAssay Description:Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-1 adrenergic receptor(Homo sapiens (Human))
UniversitÄT WÜRzburg

Curated by PDSP Ki Database
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKd:  1.76nMpH: 7.4 T: 2°CAssay Description:The whole cell-binding studies were undertaken in CHO cell lines stably expressing each beta-adrenoceptor subtype. Nonspecific binding was determined...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKd:  0.400nMAssay Description:The whole cell-binding studies were undertaken in CHO cell lines stably expressing each beta-adrenoceptor subtype. Nonspecific binding was determined...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetBeta-3 adrenergic receptor(Homo sapiens (Human))
UniversitÄT WÜRzburg

Curated by PDSP Ki Database
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKd:  5nMAssay Description:The whole cell-binding studies were undertaken in CHO cell lines stably expressing each beta-adrenoceptor subtype. Nonspecific binding was determined...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-2 adrenergic receptor(Homo sapiens (Human))
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)

Curated by ChEMBL
LigandPNGBDBM25759(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Affinity DataKd:  0.195nMAssay Description:Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintilla...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank