ChEMBL ligand: CHEMBL3265032 (Entospletinib, GS-9973, SYK INHIBITOR GS-9973)
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
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!
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/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!
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] 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!
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
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL	Inhibition of TRKA (unknown origin)	B	6.24	pIC50	569	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
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]
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL	Inhibition of BRK (unknown origin)	B	6.07	pIC50	842	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
ret proto-oncogene/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]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL	Inhibition of ROS1 (unknown origin)	B	6.07	pIC50	857	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
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	Inhibition of FLT3 (unknown origin)	B	6.52	pIC50	303	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
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]
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 (unknown origin)	B	6.84	pIC50	143	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
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]
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)	B	7.46	pIC50	35	nM	IC50	Eur J Med Chem (2024) 270: 116375-116375 [PMID:38604095]
ChEMBL	Inhibition of SYK (unknown origin)	B	7.78	pIC50	16.5	nM	IC50	J Med Chem (2023) 66: 12697-12709 [PMID:37676858]
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]
ChEMBL	Inhibition of SYK (unknown origin) by Ambit kinase assay	B	7.96	pIC50	11	nM	IC50	Eur J Med Chem (2023) 258: 115544-115544 [PMID:37300915]
ChEMBL	Inhibition of SYK (unknown origin)	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
ChEMBL	Inhibition of Syk (unknown origin) preincubated for 20 mins followed by 33P-gamma-ATP measured after 120 mins by HotSpot assay	B	7.99	pIC50	10.3	nM	IC50	Eur J Med Chem (2023) 258: 115597-115597 [PMID:37423126]
GtoPdb	-	-	8.11	pIC50	7.7	nM	IC50	J Med Chem (2014) 57: 3856-73 [PMID:24779514]
ChEMBL	Inhibition of SYK (unknown origin)	B	8.11	pIC50	7.7	nM	IC50	Bioorg Med Chem (2023) 96: 117514-117514 [PMID:37984216]
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 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]