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Found 6218 with Last Name = 'sparks' and Initial = 'r'
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM13465((2S)-N-[(1S)-1-carbamoyl-2-{4-[(5S)-1,1,3-trioxo-1...)
Affinity DataKi:  180nMAssay Description:Inhibition constant against protein-tyrosine phosphatase 1B by PNPP enzyme assayMore data for this Ligand-Target Pair
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50300305(4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2...)
Affinity DataKi:  3.40E+4nMAssay Description:Competitive inhibition of IDO1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM13467((2R)-2-{[(1S)-1-carbamoyl-2-{4-[difluoro(phosphono...)
Affinity DataIC50:  0.400nMpH: 7.0 T: 2°CAssay Description:The activity of PTP1B enzyme was assayed with 4-nitrophenyl phosphate (pNPP) as substrate. Rate of formation of the phenolate ion was monitored at 41...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50529386(CHEMBL4458634)
Affinity DataIC50:  0.930nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50529384(CHEMBL4438376)
Affinity DataIC50:  0.990nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM261330(US10092570, Example 352 | US9707233, 350)
Affinity DataIC50: <1nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM272573(US10065963, 32c | US10376513, Example 346 | US1064...)
Affinity DataIC50: <1nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM272573(US10065963, 32c | US10376513, Example 346 | US1064...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in AKT phosphorylation incubated for 2 hrs by Alexa flour 488 based FACS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM272573(US10065963, 32c | US10376513, Example 346 | US1064...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]-ATP base...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM261317(US10376513, Example 310 | US11433071, Example 311 ...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM13469(({4-[(2S)-2-carbamoyl-2-[(2S)-2-(1-{4-[difluoro(ph...)
Affinity DataIC50:  1.70nMpH: 7.0 T: 2°CAssay Description:The activity of PTP1B enzyme was assayed with 4-nitrophenyl phosphate (pNPP) as substrate. Rate of formation of the phenolate ion was monitored at 41...More data for this Ligand-Target Pair
LigandPNGBDBM50529381(CHEMBL4446120)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50529385(CHEMBL4444112)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM384664(4-((5)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrim...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  1.90nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM272573(US10065963, 32c | US10376513, Example 346 | US1064...)
Affinity DataIC50:  2nMAssay Description:Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgE antibody-induced CD63 expression by flow cast kit methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50529388(CHEMBL4443149)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  2.40nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM50529391(CHEMBL4513857)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50004547(CHEMBL2216863 | US10065963, Compound 28 | US104280...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50529390(CHEMBL4470672)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  4.20nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125913(US8765727, 16)
Affinity DataIC50:  5nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM50529383(CHEMBL4570334)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125904(US8765727, 7)
Affinity DataIC50:  6.40nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50126143(Epacadostat | INCB-024360)
Affinity DataIC50:  7.40nMAssay Description:Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrsMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125904(US8765727, 7)
Affinity DataIC50:  8.30nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM50529389(CHEMBL4440146)
Affinity DataIC50:  8.40nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125899(US8765727, 2)
Affinity DataIC50:  9.20nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM261093((2S)-3-(3-{3-[1-(4-Amino-3- methyl-1H-pyrazolo[3,4...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261094(1-[1-(5-Chloro-2-methoxy-4-methyl-3-{1-[(1-methyl-...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261095((2S)-1-(3-{3-[1-(4-Amino-3-methyl-1H-pyrazolo[3,4-...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261096(1-(1-{5-Chloro-3-[1- (cyclopropylcarbonyl)azetidin...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM570470(1-[1-(5-Chloro-2-methoxy-4- methyl-3-{1-[(5-methyl...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261098((2R)-1-(3-{3-[1-(4-Amino-3-methyl-1H-pyrazolo[3,4-...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261099(1-[(3-{3-[1-(4-Amino-3-methyl- 1H-pyrazolo[3,4-d]p...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261100(1-(3-{3-[1-(4-Amino-3-methyl-1H- pyrazolo[3,4-d]py...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261101(1-(1-{5-Chloro-2-methoxy-4- methyl-3-[1-(1H-pyrazo...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261102(US10092570, Example 125 | US10376513, Example 125 ...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261103(US10092570, Example 126 | US10646492, Example 126 ...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM261104(1-{1-[5-Chloro-3-(1-isopropylazetidin-3-yl)-2-meth...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255840(5-(3-{1-[4-amino-3-(1-methyl-1H-pyrazol-4-yl)-1H-p...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255841(5-(3-{1-[4-amino-3-(1-methyl-1H-pyrazol-3-yl)-1H-p...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255842(5-(3-{1-[4-amino-3-(1H-pyrazol-3-yl)-1H-pyrazolo[3...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255843(5-[3-(1-{4-amino-3-[1-(2-hydroxyethyl)-1H-pyrazol-...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255844(5-{3-[1-(4-amino-3-cyclopropyl-1H-pyrazolo[3,4-d]p...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM289056(US10092570, Example 57 | US10376513, Example 57 | ...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255849(5-(3-{1-[4-amino-3-(2-aminopyrimidin-5-yl)-1H-pyra...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255850(5-{3-[1-(4-amino-3-{6-[(methylamino)carbonyl]pyrid...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM255851(5-{3-[1-(4-amino-3-pyridin-4-yl-1H-pyrazolo[3,4-d]...)
Affinity DataIC50: <10nMAssay Description:The kinase reaction was conducted in polystyrene 384-well matrix white plate from Thermo Fisher Scientific in a final volume of 25 μL. Inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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