ChEMBL ligand: CHEMBL3134157
sphingosine kinase 1/Sphingosine kinase 1 in Human [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1] sphingosine kinase 1/Sphingosine kinase 1 in Mouse [ChEMBL: CHEMBL2401605] [GtoPdb: 2204] [UniProtKB: Q8CI15] There should be some charts here, you may need to enable JavaScript!
sphingosine kinase 2/Sphingosine kinase 2 in Human [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0] 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
sphingosine kinase 1/Sphingosine kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
ChEMBL	Binding affinity to SK1 (unknown origin) assessed as inhibition of sphingosine phosphorylation	B	8.3	pKd	5	nM	Kd	J Med Chem (2018) 61: 9811-9840 [PMID:29969256]
ChEMBL	Inhibition of His6 tagged human SphK1 expressed in Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins prior substrate addition by Caliper assay	B	8.37	pKi	4.3	nM	Ki	ACS Med Chem Lett (2014) 5: 1329-1333 [PMID:25516793]
ChEMBL	Inhibition of SK1 (unknown origin)	B	8.4	pKi	4	nM	Ki	J Med Chem (2016) 59: 965-984 [PMID:26780304]
GtoPdb	-	-	8.44	pKi	3.6	nM	Ki	Biochem J (2012) 444: 79-88 [PMID:22397330]
ChEMBL	Inhibition of recombinant human C-terminal His-tagged SPHK1 expressed in fall armyworm sf21 cells using sphingosine as substrate after 1 hr by FITC-based caliper assay	B	8.44	pKi	3.6	nM	Ki	J Med Chem (2017) 60: 3933-3957 [PMID:28406646]
ChEMBL	Inhibition of human C-terminal His6-tagged SphK1 expressed in baculovirus infected Sf21 insect cells	B	8.44	pKi	3.6	nM	Ki	Eur J Med Chem (2017) 139: 461-481 [PMID:28822281]
ChEMBL	Inhibition of recombinant human SphK1 expressed in baculovirus infected Sf9 cells assessed as decrease in [33P]SIP production using D-erythro-sphingosine as substrate in presence of [gamma33P]-ATP by scintillation counting method	B	8.44	pKi	3.6	nM	Ki	Bioorg Med Chem (2021) 30: 115941-115941 [PMID:33385956]
ChEMBL	Competitive inhibition of recombinant human C-terminal His-tagged SphK1 expressed in baculovirus infected Sf21 cells using varying concentrations of FITC-sphingosine as substrate incubated for 30 mins by LC-MS/MS analysis	B	8.44	pKi	3.6	nM	Ki	Eur J Med Chem (2020) 206: 112713-112713 [PMID:32919113]
ChEMBL	Competitive-inhibition of recombinant human C-terminal His6-tagged Sphk1 expressed in baculovirus infected Sf21 insect cells using varying levels of sphingosine as substrate measured after 30 mins by LC-MS analysis	B	8.44	pKi	3.6	nM	Ki	Eur J Med Chem (2021) 212: 113121-113121 [PMID:33445156]
ChEMBL	Inhibition of human recombinant SphK1 expressed in Sf9 cells assessed as radiolabeled products using 5 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting	B	8.44	pKi	3.6	nM	Ki	J Med Chem (2015) 58: 1879-1899 [PMID:25643074]
ChEMBL	Inhibition of recombinant His-tagged human SK1 assessed as production of [32P]-S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP	B	6.41	pIC50	387	nM	IC50	J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL	Inhibition of SphK1 (unknown origin)	B	7.4	pIC50	40	nM	IC50	Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967]
ChEMBL	Inhibition of recombinant SK1 (unknown origin) using sphingosine and [gamma-32P]ATP as substrate after 30 mins	B	7.55	pIC50	28	nM	IC50	Medchemcomm (2013) 4: 1394-1399 [PMID:24396570]
ChEMBL	Inhibition of SK1 (unknown origin) using 5 uM of sphingosine as substrate	B	7.55	pIC50	28	nM	IC50	J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL	Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis	B	7.55	pIC50	28	nM	IC50	J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL	Inhibition of SPHK1 in human whole-blood using C17-sphingosine as substrate assessed as reduction in C17-S1P production preincubated for 30 mins followed by substrate addition measured after 10 mins by MS analysis	B	7.7	pIC50	20	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL	Inhibition of SK1 (unknown origin) using 3 uM of sphingosine as substrate	B	8.52	pIC50	3	nM	IC50	J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL	Inhibition of recombinant C-terminal His6-tagged human SphK1 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay	B	8.57	pIC50	2.7	nM	IC50	Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190]
ChEMBL	Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in S1P formation using sphingosine as substrate after 1 hr by FITC-based caliper assay	B	8.57	pIC50	2.7	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
GtoPdb	-	-	8.57	pIC50	2.7	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL	Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in ADP formation using sphingosine as substrate preincubated for 15 mins followed by substrate addition after 1 hr by transcreener-based fluorescence polarization assay	B	8.7	pIC50	2	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
GtoPdb	-	-	8.7	pIC50	2	nM	IC50	Biochem J (2012) 444: 79-88 [PMID:22397330]
ChEMBL	Inhibition of SPHK1 in human MDA1483 cells using C17-sphingosine as substrate assessed as reduction in C17-S1P formation preincubated for 30 mins with substrate measured after 15 mins by LC-MS analysis	B	9.1	pIC50	0.8	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
sphingosine kinase 1/Sphingosine kinase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2401605] [GtoPdb: 2204] [UniProtKB: Q8CI15]
ChEMBL	Inhibition of SphK1 in mouse erythrocytes using sphingosine as substrate by luminescence assay	B	8.44	pKi	3.6	nM	Ki	ACS Med Chem Lett (2016) 7: 229-234 [PMID:26985306]
sphingosine kinase 2/Sphingosine kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
ChEMBL	Inhibition of SK2 (unknown origin)	B	8.44	pKi	3.6	nM	Ki	J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL	Inhibition of recombinant human SK2 assessed as production of [32P] S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP relative to control	B	4.77	pIC50	17000	nM	IC50	J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL	Inhibition of SK2 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL	Inhibition of SphK2 (unknown origin)	B	5.27	pIC50	5400	nM	IC50	Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967]
ChEMBL	Inhibition of recombinant human full-length N-terminal His-tagged SK2 expressed in baculovirus infected Sf9 insect cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL	Inhibition of human recombinant C-terminal His6 tagged SphK2 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay	B	6.44	pIC50	360	nM	IC50	Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190]
ChEMBL	Inhibition of SPHK2 (unknown origin) by FITC-based caliper assay	B	6.45	pIC50	356	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
GtoPdb	-	-	6.45	pIC50	356	nM	IC50	J Med Chem (2017) 60: 2562-2572 [PMID:28231433]

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]