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ChEMBL ligand: CHEMBL3265032 (Entospletinib, GS-9973, SYK INHIBITOR GS-9973) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034798] [GtoPdb: 1805] [UniProtKB: P05532] | ||||||||
ChEMBL | Inhibition of cKit in stem cell factor-stimulated bone marrow derived mouse mast cells assessed as phosphorylation after 1 hr incubation | B | 6.35 | pEC50 | 445 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
ChEMBL | Inhibition of BTK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser | B | 6.1 | pIC50 | 801 | nM | IC50 | Eur J Med Chem (2020) 204: 112636-112636 [PMID:32731189] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation | B | 6.34 | pEC50 | 453 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
ChEMBL | Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry | B | 6.49 | pEC50 | 327 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
ChEMBL | Inhibition of Ret in human SK-M-MC cells assessed as assessed as phosphorylation after 1 hr incubation | B | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
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 assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis | B | 4.71 | pIC50 | 19416 | 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 | 6.06 | pIC50 | 878 | 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 | 6.42 | pIC50 | 377 | nM | IC50 | J Med Chem (2015) 58: 1950-1963 [PMID:25633741] |
ChEMBL | Inhibition of Syk in immune complex-stimulated human monocyte assessed as TNFalpha production after 1 hr incubation | B | 6.83 | pIC50 | 147 | nM | IC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of SYK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser | B | 7.09 | pIC50 | 82 | nM | IC50 | Eur J Med Chem (2020) 204: 112636-112636 [PMID:32731189] |
ChEMBL | Inhibition of SYK (unknown origin) using XL665-labeled peptide as substrate in presence of ATP measured after 30 mins by TR-FRET assay | B | 7.78 | pIC50 | 16.5 | nM | IC50 | ACS Med Chem Lett (2020) 11: 506-513 [PMID:32292557] |
GtoPdb | - | - | 8.11 | pIC50 | 7.7 | nM | IC50 | J Med Chem (2014) 57: 3856-73 [PMID:24779514] |
ChEMBL | Inhibition of full length Syk (unknown origin) using biotinylated peptide substrate | B | 8.11 | pIC50 | 7.7 | nM | IC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of Syk in goat antihuman IgE-induced CD63 expression in human whole blood by FACS analysis | B | 6.44 | pEC50 | 367 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of SYK in human whole blood assessed as reduction in anti-FCepsilonR1 mAb-induced basophil activation by measuring decrease in CD63 surface expression incubated for 60 mins followed by anti-FCepsilonR1 mAb stimulation for 20 mins by flow cytometry analysis | B | 6.75 | pEC50 | 178 | nM | EC50 | ACS Med Chem Lett (2020) 11: 506-513 [PMID:32292557] |
ChEMBL | Inhibition of Syk in alphaIgM-stimulated human B cells assessed as CD86 expression after 1 hr incubation by flow cytometry | B | 6.9 | pEC50 | 125 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of Syk in alphaIgM-stimulated human B cells assessed as cell proliferation after 1 hr incubation by flow cytometry | B | 7.39 | pEC50 | 41 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay | B | 7.59 | pEC50 | 26 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
ChEMBL | Inhibition of SYK in human Ramos cells assessed as reduction in antihuman IgM F(ab)2-induced phosphorylation of BLNK at Y96 residue preincubated for 1 hr followed by antihuman IgM F(ab)2 stimulation for 5 mins by MSD high bind plate assay | B | 8.7 | pEC50 | 2 | nM | EC50 | ACS Med Chem Lett (2020) 11: 506-513 [PMID:32292557] |
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4364] [GtoPdb: 2230] [UniProtKB: Q64725] | ||||||||
ChEMBL | In vitro inhibition of Syk phosphorylation in rat whole blood | B | 5.72 | pEC50 | 1900 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
ChEMBL | Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation | B | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (2014) 57: 3856-3873 [PMID:24779514] |
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]