P505-15 [Ligand Id: 8070] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2177736 (BIIB-057, P505-15, PRT-062607, PRT-2607) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG 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] |
| 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 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] |
| p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK7 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) |
| 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) |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor 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) |
| SRC proto-oncogene, non-receptor tyrosine kinase/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) |
| 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 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 | Bioorg Med Chem Lett (2015) 25: 4642-4647 [PMID:26320624] |
| 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 (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) |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Pharmacol Exp Ther (2012) 340: 350-9 [PMID:22040680] |
| 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 | 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 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] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
