General Information of the Protein
Protein ID
PT01766
Protein Name
Sphingosine kinase 1
Secondarily
Protein Name
Acetyltransferase SPHK1
Gene Name
SPHK1
Secondarily
Gene Name
SK1
SPHK
SPK
Sequence
MDPAGGPRGVLPRPCRVLVLLNPRGGKGKALQLFRSHVQPLLAEAEISFTLMLTERRNHARELVRSEELGRWDALVVMSGDGLMHEVVNGLMERPDWETAIQKPLCSLPAGSGNALAASLNHYAGYEQVTNEDLLTNCTLLLCRRLLSPMNLLSLHTASGLRLFSVLSLAWGFIADVDLESEKYRRLGEMRFTLGTFLRLAALRTYRGRLAYLPVGRVGSKTPASPVVVQQGPVDAHLVPLEEPVPSHWTVVPDEDFVLVLALLHSHLGSEMFAAPMGRCAAGVMHLFYVRAGVSRAMLLRLFLAMEKGRHMEYECPYLVYVPVVAFRLEPKDGKGVFAVDGELMVSEAVQGQVHPNYFWMVSGCVEPPPSWKPQQMPPPEEPL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Catalyzes the phosphorylation of sphingosine to form sphingosine 1-phosphate (SPP), a lipid mediator with both intra- and extracellular functions. Also acts on D-erythro-sphingosine and to a lesser extent sphinganine, but not other lipids, such as D,L-threo-dihydrosphingosine, N,N-dimethylsphingosine, diacylglycerol, ceramide, or phosphatidylinositol (PubMed:20577214, PubMed:23602659, PubMed:29662056, PubMed:24929359, PubMed:11923095). In contrast to proapoptotic SPHK2, has a negative effect on intracellular ceramide levels, enhances cell growth and inhibits apoptosis (PubMed:16118219). Involved in the regulation of inflammatory response and neuroinflammation. Via the product sphingosine 1-phosphate, stimulates TRAF2 E3 ubiquitin ligase activity, and promotes activation of NF-kappa-B in response to TNF signaling leading to IL17 secretion (PubMed:20577214). In response to TNF and in parallel to NF-kappa-B activation, negatively regulates RANTES induction through p38 MAPK signaling pathway (PubMed:23935096). Involved in endocytic membrane trafficking induced by sphingosine, recruited to dilate endosomes, also plays a role on later stages of endosomal maturation and membrane fusion independently of its kinase activity (PubMed:28049734, PubMed:24929359). In Purkinje cells, seems to be also involved in the regulation of autophagosome-lysosome fusion upon VEGFA (PubMed:25417698).
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Uniprot ID
Primary ID:
Q9NYA1

Secondarily ID:
Q8N632
Q96GK1
Q9HD92
Q9NY70
Q9NYL3
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Ensembl ID
ENSG00000176170
HGNC ID
HGNC:11240
Subcellular Location
Cytoplasm
Nucleus
Cell membrane
Endosome membrane
Membrane
Clathrin-coated pit
Synapse
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0434809
[(2R)-1-[[4-[[3-[(3-fluorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28FNO3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0554436
[3-[[4-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]phenyl]methoxy]phenyl] benzenesulfonate
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C25H27NO5S
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0540798
[(2R)-1-[[4-[(3-phenylmethoxyphenoxy)methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H29NO3
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0440434
[(2R)-1-[[4-[[3-(2-phenylethyl)phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C27H31NO2
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0109512
[(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C27H31NO4S
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0562117
[(2R)-1-[[4-[[3-[(2-chlorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28ClNO3
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0440433
[(2R)-1-[[4-[[3-[(2-fluorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28FNO3
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0440435
[(2R)-1-[[4-[[3-[(3-chlorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28ClNO3
 1
1
IC50 = 44 nM
   TI
   LI
   LO
   TS
CP0384684
[(2R)-1-[[4-[(3-benzylsulfanylphenoxy)methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H29NO2S
 1
1
IC50 = 137 nM
   TI
   LI
   LO
   TS
CP0080998
[(2R)-1-[[4-[[3-(benzenesulfonylmethyl)phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H29NO4S
 1
1
IC50 = 144 nM
   TI
   LI
   LO
   TS
CP0384682
[(2R)-1-[[4-[[3-[(4-fluorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28FNO3
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0384683
[(2R)-1-[[4-[[3-[(4-fluorophenyl)methylsulfanyl]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28FNO2S
 1
1
IC50 = 765 nM
   TI
   LI
   LO
   TS
CP0548115
[(2R)-1-[[4-[[3-[(4-chlorophenyl)methylsulfanyl]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28ClNO2S
 1
1
IC50 = 2360 nM
   TI
   LI
   LO
   TS
CP0540799
[(2R)-1-[[4-[[3-[(4-chlorophenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H28ClNO3
 1
1
IC50 = 4130 nM
   TI
   LI
   LO
   TS
CP0434810
[(2R)-1-[[4-[[3-[(4-methoxyphenyl)methoxy]phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C27H31NO4
 1
1
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0541089
4-[[3-[[4-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]phenyl]methoxy]phenoxy]methyl]benzonitrile
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C27H28N2O3
 1
1
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0424577
4-methyl-N-[3-[[2-[(4-methylphenyl)sulfonylamino]phenyl]iminomethyl]phenyl]benzenesulfonamide
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C27H25N3O4S2
 1
1
Ki = 27000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0368510
[(2R)-1-[[4-[(3-cyclohexylphenoxy)methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C25H33NO2
 1
1 IC50 = 1.5 nM
CP0109512
[(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C27H31NO4S
 8
1 IC50 = 2.6 nM
2 IC50 = 3 nM
3 IC50 = 20 nM
4 IC50 = 28 nM
5 IC50 = 40 nM
6 IC50 = 387 nM
7 Kd = 5 nM
8 Ki = 4 nM
CP0176545
(2R,4S)-1-[2-[4-[[4-[2-fluoro-5-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C24H25F4N3O2S
 1
1 IC50 = 3 nM
CP0176546
(2R,4S)-1-[2-[4-[[4-(2,4-dichlorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H25Cl2N3O2S
 1
1 IC50 = 3 nM
CP0220533
(2R,4S)-1-[2-[4-[[4-[2-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C24H25F4N3O2S
 1
1 IC50 = 4 nM
CP0100910
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino]phenyl]ethyl]piperidin-4-ol
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C24H26F3N3O2S
 1
1 IC50 = 5 nM
CP0199268
(2R,4S)-1-[2-[4-[[4-(1-adamantyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C27H37N3O2S
 1
1 IC50 = 5 nM
CP0199269
(2R,4S)-1-[2-[4-[[4-[2-fluoro-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C24H25F4N3O2S
 1
1 IC50 = 5 nM
CP0080997
(3S)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-3-ol
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C26H29NO4S
 1
1 IC50 = 5.2 nM
CP0240366
(3R,4R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidine-3,4-diol
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C26H29NO5S
 1
1 IC50 = 6.4 nM
CP0078863
(2R,4S)-1-[2-[4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H26ClN3O2S
 1
1 IC50 = 8 nM
CP0186782
(2R,4S)-1-[2-[4-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H26ClN3O2S
 1
1 IC50 = 10 nM
CP0215983
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[[4-(3-methylphenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]piperidin-4-ol
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C24H29N3O2S
 1
1 IC50 = 10 nM
CP0215985
(2R,4S)-1-[2-[4-[(4-cyclohexyl-1,3-thiazol-2-yl)amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H33N3O2S
 1
1 IC50 = 10 nM
CP0067907
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[[4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino]phenyl]ethyl]piperidin-4-ol
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C24H26F3N3O2S
 2
1 IC50 = 10 nM
2 IC50 = 20 nM
CP0103698
[(2R)-1-[[4-[(3-propan-2-ylphenoxy)methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C22H29NO2
 1
1 IC50 = 19 nM
CP0233130
(2R,4S)-1-[2-[4-[[4-(2-fluorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H26FN3O2S
 1
1 IC50 = 20 nM
CP0304537
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]piperidin-4-ol
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C24H29N3O3S
 1
1 IC50 = 30 nM
CP0080998
[(2R)-1-[[4-[[3-(benzenesulfonylmethyl)phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C26H29NO4S
 1
1 IC50 = 35 nM
CP0517809
(3R,4S)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidine-3,4-diol
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C26H29NO5S
 1
1 IC50 = 38 nM
CP0050360
(S)-2-amino-4-hydroxy-N-(4-octylphenyl)butanamide
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C18H30N2O2
 2
1 IC50 = 50 nM
2 Ki = 1400 nM
CP0225106
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]piperidin-4-ol
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C24H29N3O3S
 1
1 IC50 = 50 nM
CP0176540
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-[(4-phenyl-1,3-thiazol-2-yl)amino]phenyl]ethyl]piperidin-4-ol
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C23H27N3O2S
 1
1 IC50 = 70 nM
CP0186811
(2R,4S)-1-[2-[4-[(4-butyl-1,3-thiazol-2-yl)amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C21H31N3O2S
 1
1 IC50 = 70 nM
CP0248976
(2R,4S)-1-[2-[4-[(4-cyclopentyl-1,3-thiazol-2-yl)amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C22H31N3O2S
 1
1 IC50 = 130 nM
CP0323459
[(2R)-1-[[4-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C22H25N3O3
 1
1 IC50 = 173 nM
CP0203703
(2R,4S)-1-[2-[4-[[4-(3-fluorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H26FN3O2S
 1
1 IC50 = 320 nM
CP0176542
(2R,4S)-1-[2-[4-[[4-(4-fluorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
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C23H26FN3O2S
 1
1 IC50 = 360 nM
CP0015606
4-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol
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C15H11ClN2OS
 6
1 IC50 = 500 nM
2 IC50 = 35000 nM
3 Ki = 500 nM
4 Ki = 12000 nM
5 Ki = 16000 nM
6 Ki = 17000 nM
CP0477698
[(2S)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C27H31NO4S
 1
1 IC50 = 703 nM
CP0547860
[(2R)-1-[[4-[[3-(cyclopropylsulfonylmethyl)phenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol
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C23H29NO4S
 1
1 IC50 = 1470 nM
CP0058280
(E)-(2S,3R)-2-Dimethylamino-octadec-4-ene-1,3-diol
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C20H41NO2
 5
1 IC50 = 2170 nM
2 IC50 = 5700 nM
3 IC50 = 35790 nM
4 IC50 = 60000 nM
5 Ki = 5000 nM
CP0355652
N-[3-[[4-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]methyl]phenyl]methoxy]phenyl]benzamide
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C26H28N2O3
 1
1 IC50 > 8800 nM
CP0762701
(S)-1-(4-(4-(3-(2-Cyclohexylethyl)phenyl)oxazol-2-yl)benzoyl)pyrrolidine-2-carboximidamide Hydrochloride
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C29H35ClN4O2
 1
1 Ki = 50 nM
CP0334241
(2S)-2-[3-(4-octylphenyl)-1,2,4-oxadiazol-5-yl]pyrrolidine-1-carboximidamide
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C21H31N5O
 1
1 Ki = 1000 nM
CP0722287
N'-(1-(3,4-dimethoxyphenyl)ethylidene)-3-(4-methoxyphenyl)-1H-pyrazole-5-carbohydrazide
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C21H22N4O4
 1
1 Ki = 1330 nM
CP0070490
(E,2R,3S)-2-(methylamino)-5-(4-pentylphenyl)pent-4-ene-1,3-diol
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C17H27NO2
 1
1 Ki = 10000 nM
CP0709550
(S)-2-(3-(4-Octylphenyl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide Hydrochloride
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C21H32ClN5O
 2
1 Ki = 13300 nM
2 Ki = 16000 nM
CP0352767
4-methyl-N-[2-[[2-[(4-methylphenyl)sulfonylamino]phenyl]iminomethyl]phenyl]benzenesulfonamide
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C27H25N3O4S2
 1
1 Ki = 27000 nM
Clinical Information about the Protein
Target 1 ( Sphingosine kinase 1 (SPHK1) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Ovarian cancer [ICD-11: 2C73]
2 Drug abuse [ICD-11: 6C4G.1Z]
3 Vascular disease [ICD-11: BE2Z]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Phenoxodiol Phase 1/2
Ovarian cancer
2 GSK618334 Phase 1
Drug abuse
Investigative Drug(s) 1 Investigative Drug  1
1 VPC-94075 Investigative
Vascular disease