ChEMBL ligand: CHEMBL3265032 (Entospletinib, GS-9973, SYK INHIBITOR GS-9973)
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Mouse [ChEMBL: CHEMBL2034798] [GtoPdb: 1805] [UniProtKB: P05532] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Rat [ChEMBL: CHEMBL4364] [GtoPdb: 2230] [UniProtKB: Q64725] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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]