P505-15 [Ligand Id: 8070] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2177736 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| GtoPdb | - | - | 7.06 | pIC50 | 88 | nM | IC50 | J Pharmacol Exp Ther (2012) 340: 350-9 [PMID:22040680] |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 7.22 | pIC50 | 60 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of human PKCalpha | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.61 | pIC50 | 244 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.86 | pIC50 | 139 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.86 | pIC50 | 139 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286] | ||||||||
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.78 | pIC50 | 166 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| GtoPdb | - | - | 7.09 | pIC50 | 81 | nM | IC50 | J Pharmacol Exp Ther (2012) 340: 350-9 [PMID:22040680] |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 7.09 | pIC50 | 81 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 5.76 | pIC50 | 1750 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.52 | pIC50 | 300 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.52 | pIC50 | 300 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of Lyn (unknown origin) | B | 6.62 | pIC50 | 238 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.7 | pIC50 | 199 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of Syk in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.44 | pIC50 | 3631.8 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.47 | pIC50 | 3389.4 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.52 | pIC50 | 3021 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.61 | pIC50 | 2455.7 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.63 | pIC50 | 2345.2 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes in presence of 90% human blood assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis | B | 6.02 | pIC50 | 952 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4642-4647 [PMID:26320624] |
| ChEMBL | Inhibition of Syk in human whole blood assessed as inhibition of P-SLP76 in CD14+ monocytes by flow cytometry | B | 6.02 | pIC50 | 952 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| ChEMBL | Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis | B | 6.02 | pIC50 | 952 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of SYK in human whole blood | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2013) 56: 1677-1692 [PMID:23350847] |
| ChEMBL | Inhibition of SYK in human Ramos cells | B | 6.65 | pIC50 | 223 | nM | IC50 | J Med Chem (2013) 56: 1677-1692 [PMID:23350847] |
| ChEMBL | Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay | B | 6.75 | pIC50 | 178 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| ChEMBL | Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis | B | 6.75 | pIC50 | 178 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis | B | 6.75 | pIC50 | 178 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4642-4647 [PMID:26320624] |
| ChEMBL | Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4642-4647 [PMID:26320624] |
| ChEMBL | Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of Syk (unknown origin) using 4 uM peptide assessed as product formation after 60 mins incubation by microfluidic mobility shift assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| ChEMBL | Inhibition Assay: SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). LANCE refers to homogeneous time resolved fluorometry applications using techniques such as time-resolved fluorescence resonance energy transfer assay (TR-FRET) (see generally for procedures in Perkin Elmer Application Note How to Optimize a Tyrosine Kinase Assay Using Time Resolved Fluorescence-Based LANCE Detection, wwww.perkinelmer.com/lifesciences). The assay principle involves detection of a phosphorylated substrate using energy transfer from a phosphospecific europium-labeled antibody to streptavidin-allophycocyanin as an acceptor.To test the ability of candidate molecules to inhibit SYK tyrosine phosphorylation activity, molecules are reconstituted in 30% DMSO and serially diluted 1:3 with the final dilution containing DMSO in the absence of the candidate molecule. The final DMSO concentration in the assay is 3%. | B | 8.22 | pIC50 | 6 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| ChEMBL | In Vitro Assay: Potency of candidate molecules for inhibiting syk tyrosine phosphorylation activity is assessed by measuring the ability of a test compound to inhibit syk-mediated tyrosine phosphorylation of a syk-specific substrate.SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). LANCE refers to homogeneous time resolved fluorometry applications using techniques such as time-resolved fluorescence resonance energy transfer assay (TR-FRET) (see generally for procedures in Perkin Elmer Application Note How to Optimize a Tyrosine Kinase Assay Using Time Resolved Fluorescence-Based LANCE Detection, wwww.perkinelmer.com/lifesciences). The assay principle involves detection of a phosphorylated substrate using energy transfer from a phosphospecific europium-labeled antibody to streptavidin-allophycocyanin as an acceptor.To test the ability of candidate molecules to inhibit SYK tyrosine phosphorylation activity, molecules are reconstituted in 30% DMSO and serially diluted 1:3 with the final dilution containing DMSO in the absence of the candidate molecule. The final DMSO concentration in the assay is 3%. Kinase assays are performed as a two part reaction. The first reaction is a kinase reaction and which comprises of a candidate molecule, full length active recombinant SYK enzyme (Millipore, Calif.) and biotin-labeled SYK-specific substrate biotin-DEEDYESP-OH. The second reaction involves termination of the kinase reaction and the simultaneous addition of the detection reagents-europium-labeled anti-phosphotyrosine reagent (Eu-W1024-PY100, Perkin Elmer, Boston, Mass.) and Streptavidin-Allophycocyanin detection reagent (SA-APC, Prozyme, Calif.). The kinase reaction is performed in a black U-bottom 96-well microtitre plate. The final reaction volume is 50 ÎĽL and contains a final concentration of 1 nM active SYK enzyme, 550 nM SYK-substrate, and 100 ÎĽM ATP diluted in a buffer containing 50 mM Tris pH 7.5, 5 mM MgCl2, and 1 mM DTT. The reaction is allowed to proceed for 1 hour at room temperature. The quench buffer contains 100 mM Tris pH 7.5, 300 mM NaCl2, 20 mM EDTA, 0.02% Brij35, and 0.5% BSA. The detection reagents are added to the reaction mixture at the following dilutions 1:500 for Eu-W1024-PY100 and 1:250 for SA-APC. The kinase reaction is terminated by the addition of 50 ÎĽL quench buffer containing the detection reagents. The detection is allowed to proceed for 1 hr at room temperature. Detection of the phosphorlated substrate in the absence and presence of inhibitors is measured in the TR-FRET instrument, Analyst HT (Molecular Probes, Sunnyvale, Calif.) and the condition for measurements are set up using CriterionHost Release 2.0 (Molecular Probes, Sunnyvale, Calif.). The settings used are a follows: excitation 360 nm, emission 665-7.5 nm, beam splitter 350 nm 50/50, flash 100 pulses, delay 60 us, integration 400 us, z-height 2 mm. Inhibition of SYK-tyrosine kinase activity is calculated as the maximum response observed in the presence of inhibitor, compared to that in the absence of inhibitor. IC50s were derived by non-linear regression analysis. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-9579320-B2. Inhibitors of syk and JAK protein kinases (2017) |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Pharmacol Exp Ther (2012) 340: 350-9 [PMID:22040680] |
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 9 | pIC50 | 1 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| ChEMBL | Inhibition of human recombinant truncated SYK (360 to 365 amino acid residues) using N-terminally biotinylated EPEGDYEEVLE peptide as substrate assessed as inhibition of [33P]-ATP incorporation incubated for 10 mins prior to substrate addition measured after 15 mins by scintillation counting | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2013) 56: 1677-1692 [PMID:23350847] |
| ChEMBL | Inhibition of human recombinant spleen tyrosine kinase (360 to 635 amino acid residues) after 10 mins by scintillation counting analysis | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2012) 55: 10414-10423 [PMID:23151054] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Millipore Kinase Panel Assay: Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. | B | 6.91 | pIC50 | 123 | nM | IC50 | US-8952027-B2. Inhibitors of syk and JAK protein kinases (2015) |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-CD3 stimulation measured after 2 mins by FACS analysis | B | 5.74 | pIC50 | 1805 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of human ZAP70 | B | 7.17 | pIC50 | 68 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of ZAP70 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by manual patch clamp assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
| ChEMBL | Inhibition of human ERG channel | B | 5.04 | pIC50 | 9100 | nM | IC50 | J Med Chem (2013) 56: 1677-1692 [PMID:23350847] |
| ChEMBL | Inhibition of human ERG by Q-patch assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2278-2282 [PMID:24726806] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
