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Found 189 with Last Name = 'crouse' and Initial = 'k'
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.0269nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase TXK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.131nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.545nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.679nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.31nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466891(CHEMBL4281109)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466897(CHEMBL4287715)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  32.4nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466893(CHEMBL4291727)
Affinity DataKi:  50nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  62.3nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466892(CHEMBL4283871)
Affinity DataKi:  1.20E+3nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50406141(CHEMBL5286547)
Affinity DataKi:  1.80E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406139(CHEMBL5281816)
Affinity DataKi:  3.60E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406140(CHEMBL5284779)
Affinity DataKi:  4.00E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406144(CHEMBL5283506)
Affinity DataKi:  1.10E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406145(CHEMBL5287800)
Affinity DataKi:  1.70E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406143(CHEMBL5287916)
Affinity DataKi:  1.90E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466913(CHEMBL4289304)
Affinity DataKi:  1.90E+4nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50406142(CHEMBL5280788)
Affinity DataKi:  3.70E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataIC50:  0.346nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  0.960nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM159756(PF-02384554 | US10966980, Example 8 | US9035074, 8)
Affinity DataIC50:  1nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  2.60nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM159756(PF-02384554 | US10966980, Example 8 | US9035074, 8)
Affinity DataIC50:  2.70nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  3.10nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466890(CHEMBL4290728)
Affinity DataIC50:  3.30nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189877(US10227346, Example 5 | US10426135, Example 5 | US...)
Affinity DataIC50:  4.10nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466912(CHEMBL4283051)
Affinity DataIC50:  4.80nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466897(CHEMBL4287715)
Affinity DataIC50:  5nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466890(CHEMBL4290728)
Affinity DataIC50:  5nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466891(CHEMBL4281109)
Affinity DataIC50:  5nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466893(CHEMBL4291727)
Affinity DataIC50:  5.5nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC5a anaphylatoxin chemotactic receptor 1(Homo sapiens (Human))
Wyeth Research

Curated by ChEMBL
LigandPNGBDBM50305735(CHEMBL595990 | N,N'-(1,2-phenylene)bis(N-methyl-1-...)
Affinity DataIC50:  6.70nMAssay Description:Antagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 min...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466914(CHEMBL4283312)
Affinity DataIC50:  7.60nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466915(CHEMBL4282848)
Affinity DataIC50:  7.90nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189877(US10227346, Example 5 | US10426135, Example 5 | US...)
Affinity DataIC50:  9.5nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189922(US10227346, Example 109 | US10426135, Example 109 ...)
Affinity DataIC50:  10nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466908(CHEMBL4283530)
Affinity DataIC50:  10nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466895(CHEMBL4281170)
Affinity DataIC50:  11nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466911(CHEMBL4288376)
Affinity DataIC50:  13nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466909(CHEMBL4284588)
Affinity DataIC50:  13nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466908(CHEMBL4283530)
Affinity DataIC50:  13nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189909(US10227346, Example 33 | US10426135, Example 33 | ...)
Affinity DataIC50:  14nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  15nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466907(CHEMBL4291498)
Affinity DataIC50:  15nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466910(CHEMBL4292862)
Affinity DataIC50:  16nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189909(US10227346, Example 33 | US10426135, Example 33 | ...)
Affinity DataIC50:  18nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466899(CHEMBL4295241)
Affinity DataIC50:  20nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM189923(US10227346, Example 110 | US10426135, Example 110 ...)
Affinity DataIC50:  20nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466904(CHEMBL4286366)
Affinity DataIC50:  20nMAssay Description:Inverse agonist activity at human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cells assessed as inhibi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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