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Found 3607 with Last Name = 'gosmini' and Initial = 'r'
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataKi:  30nMAssay Description:Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (un...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  0.251nMAssay Description:Binding affinity to full-length BRD4 short isoform (unknown origin) by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  0.398nMAssay Description:Inhibition of human BRD4 bromodomain 1 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  0.398nMAssay Description:Inhibition of human BRD4 bromodomain 1/2 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548398(CHEMBL3718309)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-sti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  0.631nMAssay Description:Inhibition of human BRD3 bromodomain 1 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain and PHD finger-containing protein 3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50: <1nMAssay Description:Inhibition of human BRPF3 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 7(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50: <1.30nMAssay Description:Inhibition of human BRD7 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  2nMAssay Description:Inhibition of human BRD3 bromodomain 2 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM194644(US9206139, 3)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant ADAMTS4 using synthetic peptide as substrate by FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM194644(US9206139, 3)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant ADAMTS5 using synthetic peptide as substrate by FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target72 kDa type IV collagenase(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379774(US9926281, Compound 279 | US9926281, Compound 448)
Affinity DataIC50:  2nMAssay Description:MMP2: Protocol 2: The basis for the assay is the cleavage of the substrate 390 MMP FRET substrate I (Anaspec, Catalog n#: AS-27076) by human MMP2 (R&...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human BRD2 bromodomain 2 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human BRD4 bromodomain 2 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeregrin(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50028142(CHEMBL2177300)
Affinity DataIC50: <4nMAssay Description:Inhibition of human BRPF1 by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379670(US9926281, Compound 194 | US9926281, Compound 413)
Affinity DataIC50:  5nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548387(CHEMBL4794652)
Affinity DataIC50:  5nMAssay Description:Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-sti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379686(US9926281, Compound 212)
Affinity DataIC50:  5nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCollagenase 3(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379776(US9926281, Compound 234)
Affinity DataIC50:  5.60nMAssay Description:MMP-13:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP13 (Chemicon, Cat #CC06...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379668(US9926281, Compound 192 | US9926281, Compound 411)
Affinity DataIC50:  6nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548393(CHEMBL3716446)
Affinity DataIC50:  6nMAssay Description:Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379681(US9926281, Compound 207 | US9926281, Compound 416)
Affinity DataIC50:  6nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMatrix metalloproteinase-14(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379776(US9926281, Compound 234)
Affinity DataIC50:  7nMAssay Description:MMP-14:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP14 (Biomol, Cat #SE-259...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379669(US9926281, Compound 193 | US9926281, Compound 412)
Affinity DataIC50:  7nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379653(US9926281, Compound 176)
Affinity DataIC50:  7nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMatrix metalloproteinase-14(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379901(US9926281, Compound 396)
Affinity DataIC50:  7nMAssay Description:MMP-14:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP14 (Biomol, Cat #SE-259...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548393(CHEMBL3716446)
Affinity DataIC50:  8nMAssay Description:Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-sti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50575720(CHEMBL4864283)
Affinity DataIC50:  8nMAssay Description:Inhibition of human recombinant ADAMTS5 using synthetic peptide as substrate by FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548412(CHEMBL4776061)
Affinity DataIC50:  8nMAssay Description:Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-sti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548406(CHEMBL4757870)
Affinity DataIC50: >10nMAssay Description:Inhibition of recombinant human PDE4A overexpressed in HEK293 cells assessed as reduction in cAMP hydrolysis by HTRF based immunoassayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379645(US9926281, Compound 167 | US9926281, Compound 408)
Affinity DataIC50:  10nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379668(US9926281, Compound 192 | US9926281, Compound 411)
Affinity DataIC50:  11nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379670(US9926281, Compound 194 | US9926281, Compound 413)
Affinity DataIC50:  11nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379649(US9926281, Compound 172 | US9926281, Compound 409)
Affinity DataIC50:  11nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548412(CHEMBL4776061)
Affinity DataIC50:  11nMAssay Description:Antagonist activity at recombinant human GPR84 receptor expressed in HEK293 cells co-expressing GNAO1 transcription variant 1 assessed as reduction i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379678(US9926281, Compound 204)
Affinity DataIC50:  11nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379668(US9926281, Compound 192 | US9926281, Compound 411)
Affinity DataIC50:  11nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379670(US9926281, Compound 194 | US9926281, Compound 413)
Affinity DataIC50:  11nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379667(US9926281, Compound 191)
Affinity DataIC50:  11nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379686(US9926281, Compound 212)
Affinity DataIC50:  12nMAssay Description:Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379975(US9926281, Compound 436)
Affinity DataIC50:  12nMAssay Description:Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379686(US9926281, Compound 212)
Affinity DataIC50:  12nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379681(US9926281, Compound 207 | US9926281, Compound 416)
Affinity DataIC50:  12nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379681(US9926281, Compound 207 | US9926281, Compound 416)
Affinity DataIC50:  12nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471902((5R)-5-[3-[(3S)- 4-(4-chloro-3- methoxy-phenyl)- 3...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471903((5R)-5-[3-[4-(4- chloro-3,5- dimethoxy- phenyl) pi...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471905((5R)-5-[3-[(3S)-4- (4-chloro-3,5- dimethoxy- pheny...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471907((5R)-5-[3-[4-(4- chloro-3-fluoro- 5-methoxy- pheny...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471908((5R)-5-[3-[(3S)-4- (4-chloro- 3-fluoro- 5-methoxy-...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM471909((5R)-5-[3-[4-(3,4- dichloro-5- methoxy- phenyl) pi...)
Affinity DataIC50:  12.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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