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Found 553 with Last Name = 'briel' and Initial = 'd'
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120151(US8697696, 8)
Affinity DataKi:  2.60nM ΔG°:  -45.5kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120150(US8697696, 7)
Affinity DataKi:  6.20nM ΔG°:  -43.5kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120152(US8697696, 9)
Affinity DataKi:  6.80nM ΔG°:  -43.3kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120149(US8697696, 6)
Affinity DataKi:  11.3nM ΔG°:  -42.2kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120154(US8697696, 11)
Affinity DataKi:  12.7nM ΔG°:  -41.9kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120146(US8697696, 3)
Affinity DataKi:  15.7nM ΔG°:  -41.4kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120153(US8697696, 10)
Affinity DataKi:  20.7nM ΔG°:  -40.8kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120147(US8697696, 4)
Affinity DataKi:  22.2nM ΔG°:  -40.6kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120144(US8697696, 1)
Affinity DataKi:  28.8nM ΔG°:  -40.0kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120148(US8697696, 5)
Affinity DataKi:  43.2nM ΔG°:  -39.1kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-5(Homo sapiens (Human))
Roche Palo Alto

US Patent
LigandPNGBDBM120145(US8697696, 2)
Affinity DataKi:  45.3nM ΔG°:  -39.0kJ/molepH: 7.5 T: 2°CAssay Description:Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a conc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin K(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50260351(CHEMBL4086667)
Affinity DataIC50:  1nMAssay Description:Inhibition of human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50260350(CHEMBL4078089)
Affinity DataIC50:  3nMAssay Description:Inhibition of human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319434((R)-3-(1'-(4,6-dimethylpyrimidine-5-carbonyl)-4'-m...)
Affinity DataIC50:  6nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310731(4-butyl-3-(cyclohexylmethyl)-8-(1-(4,6-dimethylpyr...)
Affinity DataIC50:  7nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319451((R)-3-(1'-(4,6-dimethylpyrimidine-5-carbonyl)-4'-m...)
Affinity DataIC50:  8nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310730(4-butyl-3-(cyclohexylmethyl)-8-(1-(2,6-dimethylben...)
Affinity DataIC50:  10nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310747((5S)-5-butyl-9-(1-(2,4-dimethylnicotinoyl)-4-methy...)
Affinity DataIC50:  10nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254720((4-(7-butyl-9-(morpholinosulfonyl)-3,9-diazaspiro[...)
Affinity DataIC50:  11nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310744((S)-5-butyl-9-(1-(4,6-dimethyl-2-oxo-2H-pyran-5-ca...)
Affinity DataIC50:  12nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319447((R)-4,6-dimethyl-5-(4'-methyl-4-(2-oxo-5-phenyl-3-...)
Affinity DataIC50:  12nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319442((R)-4,6-dimethyl-5-(4'-methyl-4-(2-oxo-5-(pyridin-...)
Affinity DataIC50:  12nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophosphatidic acid receptor 1(Homo sapiens (Human))
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398095(CHEMBL2182043 | US9321738, 2)
Affinity DataIC50:  18nMT: 2°CAssay Description:Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilut...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysophosphatidic acid receptor 1(Homo sapiens (Human))
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398094(CHEMBL2182044 | US9321738, 11)
Affinity DataIC50:  18nMT: 2°CAssay Description:Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilut...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysophosphatidic acid receptor 1(Homo sapiens (Human))
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398093(CHEMBL2182046 | US9321738, 6)
Affinity DataIC50:  18nMT: 2°CAssay Description:Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilut...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310726(4-butyl-3-(cyclopentylmethyl)-8-(1-(2,6-dimethylbe...)
Affinity DataIC50:  18nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254677((4-(7-butyl-9-(pyridin-2-ylsulfonyl)-3,9-diazaspir...)
Affinity DataIC50:  18nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophosphatidic acid receptor 1(Homo sapiens (Human))
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398091(CHEMBL2182049 | US9321738, 12)
Affinity DataIC50:  18.8nMT: 2°CAssay Description:Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilut...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254748((R)-(4-(7-butyl-9-(2,2,2-trifluoroethylsulfonyl)-3...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254752(1-butyl-9-(1-(4,6-dimethylpyrimidine-5-carbonyl)-4...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254675((4-(7-butyl-9-(phenylsulfonyl)-3,9-diazaspiro[5.5]...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319448((R)-3-(1'-(4,6-dimethylpyrimidine-5-carbonyl)-4'-m...)
Affinity DataIC50:  20nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319453((R)-3-(1'-(4,6-dimethylpyrimidine-5-carbonyl)-4'-m...)
Affinity DataIC50:  20nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319446((R)-4,6-dimethyl-5-(4'-methyl-4-(2-oxo-5-phenyl-3-...)
Affinity DataIC50:  21nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254718((4-(7-butyl-9-(tetrahydro-2H-pyran-4-ylsulfonyl)-3...)
Affinity DataIC50:  22nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310743((S)-5-(4-(5-butyl-3-methyl-2-oxo-1-oxa-3,9-diazasp...)
Affinity DataIC50:  22nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254716((4-(7-butyl-9-(cyclopropylsulfonyl)-3,9-diazaspiro...)
Affinity DataIC50:  22nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310727(4-butyl-8-(1-(2,6-dimethylbenzoyl)piperidin-4-yl)-...)
Affinity DataIC50:  24nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319443((R)-4,6-dimethyl-5-(4'-methyl-4-(3-methyl-2-oxo-5-...)
Affinity DataIC50:  24nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310742((+/-)-5-(4-(5-butyl-2-oxo-3-((tetrahydro-2H-pyran-...)
Affinity DataIC50:  24nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophosphatidic acid receptor 1(Homo sapiens (Human))
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398090(CHEMBL2182050 | US9321738, 13)
Affinity DataIC50:  24.5nMT: 2°CAssay Description:Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilut...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310737(5-butyl-9-(1-(4,6-dimethylpyrimidine-5-carbonyl)-4...)
Affinity DataIC50:  25nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310739((S)-5-butyl-9-(1-(4,6-dimethylpyrimidine-5-carbony...)
Affinity DataIC50:  25nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319441(5-(4-((R)-3-((trans-4-ethoxycyclohexyl)methyl)-2-o...)
Affinity DataIC50:  25nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254715((4-(7-butyl-9-(methylsulfonyl)-3,9-diazaspiro[5.5]...)
Affinity DataIC50:  25nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319449((R)-methyl 4-((3-(1'-(4,6-dimethylpyrimidine-5-car...)
Affinity DataIC50:  26nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319445((R)-4-((3-(1'-(6-cyano-2,4-dimethylnicotinoyl)-4'-...)
Affinity DataIC50:  26nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50254719((4-(7-butyl-9-(1-methyl-1H-imidazol-4-ylsulfonyl)-...)
Affinity DataIC50:  27nMAssay Description:Antagonist activity at CCR5 receptor (unknown origin) by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50319452((S)-3-(1'-(4,6-dimethylpyrimidine-5-carbonyl)-4'-m...)
Affinity DataIC50:  27nMAssay Description:Binding affinity at CCR5 receptor by radiolabelled RANTES binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 5(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50310746((5S)-5-butyl-3-((4,4-difluorocyclohexyl)methyl)-9-...)
Affinity DataIC50:  27nMAssay Description:Displacement of [125I]RANTES from human CCR5 receptor cotransfected with Galphai6 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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