General Information of the Protein
Protein ID
PT01014
Protein Name
Caspase-3
Secondarily
Protein Name
Apopain
Cysteine protease CPP32
Protein Yama
SREBP cleavage activity 1
Gene Name
CASP3
Secondarily
Gene Name
CPP32
Sequence
MENTENSVDSKSIKNLEPKIIHGSESMDSGISLDNSYKMDYPEMGLCIIINNKNFHKSTGMTSRSGTDVDAANLRETFRNLKYEVRNKNDLTREEIVELMRDVSKEDHSKRSSFVCVLLSHGEEGIIFGTNGPVDLKKITNFFRGDRCRSLTGKPKLFIIQACRGTELDCGIETDSGVDDDMACHKIPVEADFLYAYSTAPGYYSWRNSKDGSWFIQSLCAMLKQYADKLEFMHILTRVNRKVATEFESFSFDATFHAKKQIPCIVSMLTKELYFYH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Cysteine protease
>
Cysteine protease CD clan
>
Cysteine protease C14 family
Function
Thiol protease that acts as a major effector caspase involved in the execution phase of apoptosis (PubMed:7596430, PubMed:18723680, PubMed:20566630, PubMed:23650375, PubMed:35338844, PubMed:35446120). Following cleavage and activation by initiator caspases (CASP8, CASP9 and/or CASP10), mediates execution of apoptosis by catalyzing cleavage of many proteins (PubMed:7596430, PubMed:18723680, PubMed:20566630, PubMed:23650375). At the onset of apoptosis, it proteolytically cleaves poly(ADP-ribose) polymerase PARP1 at a '216-Asp-|-Gly-217' bond (PubMed:7774019, PubMed:7596430, PubMed:10497198, PubMed:16374543). Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop-helix leucine zipper domain and the membrane attachment domain (By similarity). Cleaves and activates caspase-6, -7 and -9 (PubMed:7596430). Involved in the cleavage of huntingtin (PubMed:8696339). Triggers cell adhesion in sympathetic neurons through RET cleavage (PubMed:21357690). Cleaves and inhibits serine/threonine-protein kinase AKT1 in response to oxidative stress (PubMed:23152800). Acts as an inhibitor of type I interferon production during virus-induced apoptosis by mediating cleavage of antiviral proteins CGAS, IRF3 and MAVS, thereby preventing cytokine overproduction (PubMed:30878284). Also involved in pyroptosis by mediating cleavage and activation of gasdermin-E (GSDME) (PubMed:35446120, PubMed:35338844). Cleaves XRCC4 and phospholipid scramblase proteins XKR4, XKR8 and XKR9, leading to promote phosphatidylserine exposure on apoptotic cell surface (PubMed:23845944, PubMed:33725486).
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Uniprot ID
Primary ID:
P42574

Secondarily ID:
A8K5M2
D3DP53
Q96AN1
Q96KP2
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Ensembl ID
ENSG00000164305
HGNC ID
HGNC:1504
Subcellular Location
Cytoplasm
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: CL000038 , B16-F10
Compound ID Compound Name Compound Formula
CP0036823
(-)-etoposide
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C29H32O13
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0050273
(S)-1-((1-(2-Fluoroethyl)-1H-[1,2,3]-triazol-4-yl)methyl)-5-(2(2,4-difluorophenoxymethyl)-pyrrolidine-1-sulfonyl)isatin
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C24H22F3N5O5S
 3
1 EC50 = 0.5 nM
2 IC50 = 0.5 nM
3 IC50 = 10.8 nM
CP0138925
(S)-1-((1-(2-Fluoroethyl)-1H-[1,2,3]-triazol-4-yl)methyl)-5-(2-phenoxymethyl-pyrrolidine-1-sulfonyl)isatin
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C24H24FN5O5S
 3
1 EC50 = 16.7 nM
2 IC50 = 12.2 nM
3 IC50 = 16.7 nM
CP0096205
(S)-1-Benzyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl}isatin
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C26H24N2O5S
 6
1 EC50 = 41.8 nM
2 IC50 = 2.5 nM
3 IC50 = 12.2 nM
4 IC50 = 12.3 nM
5 IC50 = 14.5 nM
6 Ki = 1.2 nM
CP0210512
CID6851947
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C23H28N4O2
 3
1 EC50 = 4080 nM
2 IC50 = 3200 nM
3 IC50 > 100000 nM
CP0045095
(S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-(phenoxymethyl)pyrrolidin-1-ylsulfonyl)indoline-2,3-dione
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C28H27FN2O6S
 4
1 IC50 = 0.3 nM
2 IC50 = 9.7 nM
3 IC50 = 9.772 nM
4 Ki = 0.2 nM
CP0057628
(S)-1-Methyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl}isatin
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C20H20N2O5S
 7
1 IC50 = 2.4 nM
2 IC50 = 114 nM
3 IC50 = 119.2 nM
4 IC50 = 120.23 nM
5 IC50 = 10000 nM
6 Ki = 15 nM
7 Ki = 56.1 nM
CP0036627
(S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-((pyridin-3-yloxy)methyl)pyrrolidin-1-ylsulfonyl)indoline-2,3-dione
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C27H26FN3O6S
 1
1 IC50 = 3.1 nM
CP0050270
(S)-1-(4-methoxybenzyl)-5-(2-((pyridin-3-yloxy)methyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C25H23N3O6S
 1
1 IC50 = 3.3 nM
CP0050269
(S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-((pyridin-3-yloxy)methyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C26H24FN3O6S
 1
1 IC50 = 3.6 nM
CP0202684
1-(4-Methoxybenzyl)-5-(2-(pyridin-3-yl-oxymethyl)-pyrolidine-1-sulfonyl)-1H-indole-2,3-dione
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C26H25N3O6S
 2
1 IC50 = 3.89 nM
2 IC50 = 3.9 nM
CP0271903
(S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methyl)-5-(2-((pyridin-3-yloxy)methyl)pyrrolidin-1-ylsulfonyl)indoline-2,3-dione
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C23H23FN6O5S
 1
1 IC50 = 4.5 nM
CP0164457
(S)-1-Allyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl}isatin
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C22H22N2O5S
 1
1 IC50 = 4.6 nM
CP0239513
(S)-1-(Cyclohexylmethyl)-5-{1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl}isatin
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C26H30N2O5S
 1
1 IC50 = 5.2 nM
CP0166997
1-Benzyl-5-(2-(pyridin-3-yl-oxymethyl)-pyrrolidine-1-sulfonyl)-1H-indole-2,3-dione
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C25H23N3O5S
 2
1 IC50 = 5.2 nM
2 IC50 = 5.248 nM
CP0297684
(S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methyl)-5-(2-((pyridin-3-yloxy)methyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C22H21FN6O5S
 1
1 IC50 = 5.6 nM
CP0061807
(S)-1-(4-Methoxybenzyl)-5-(2-phenoxymethyl-azetidine-1-sulfonyl)-1H-indole-2,3-dione
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C26H24N2O6S
 2
1 IC50 = 8.318 nM
2 IC50 = 8.4 nM
CP0219109
(S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-(phenoxymethyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C27H25FN2O6S
 1
1 IC50 = 8.6 nM
CP0057625
(S)-1-Benzyl-5-(2-phenoxymethyl-azetidine-1-sulfonyl)-1H-indole-2,3-dione
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C25H22N2O5S
 2
1 IC50 = 9.7 nM
2 IC50 = 9.772 nM
CP0160303
(S)-1-(4-(2-(2-fluoroethoxy)ethoxy)benzyl)-5-(2-(phenoxymethyl)pyrrolidin-1-ylsulfonyl)indoline-2,3-dione
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C30H31FN2O7S
 1
1 IC50 = 10.9 nM
CP0050278
(S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methyl)-5-(2-(phenoxymethyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C23H22FN5O5S
 1
1 IC50 = 11 nM
CP0050280
(S)-5-(2-((2,4-difluorophenoxy)methyl)azetidin-1-ylsulfonyl)-1-(4-(2-fluoroethoxy)benzyl)indoline-2,3-dione
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C27H23F3N2O6S
 1
1 IC50 = 12 nM
CP0287558
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C25H39N5O10
 1
1 IC50 = 12 nM
CP0050282
(S)-5-(2-((2,4-difluorophenoxy)methyl)azetidin-1-ylsulfonyl)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methyl)indoline-2,3-dione
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C23H20F3N5O5S
 1
1 IC50 = 13.4 nM
CP0050272
(S)-1-(4-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)benzyl)-5-(2-(phenoxymethyl)pyrrolidin-1-ylsulfonyl)indoline-2,3-dione
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C32H35FN2O8S
 1
1 IC50 = 13.7 nM
CP0303941
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C23H37N5O10
 1
1 IC50 = 15 nM
CP0050281
(S)-5-(2-((2,4-difluorophenoxy)methyl)pyrrolidin-1-ylsulfonyl)-1-(4-(2-fluoroethoxy)benzyl)indoline-2,3-dione
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C28H25F3N2O6S
 1
1 IC50 = 15.2 nM
CP0040399
(S)-5-{1-[2-(Phenoxymethyl)pyrrolidinyl]sulfonyl}isatin
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C19H18N2O5S
 6
1 IC50 = 16.9 nM
2 IC50 = 44 nM
3 IC50 = 239.88 nM
4 IC50 = 240 nM
5 Ki = 8.3 nM
6 Ki = 15 nM
CP0109320
1-Methyl-5-(2-(pyridin-3-yl-oxymethyl)-pyrrolidine-1-sulfonyl)--1H-indole-2,3-dione
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C19H19N3O5S
 2
1 IC50 = 23.3 nM
2 IC50 = 23.44 nM
CP0310716
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]piperidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C26H41N5O10
 1
1 IC50 = 26 nM
CP0050268
(S)-1-(4-(2-(2-fluoroethoxy)ethoxy)benzyl)-5-(2-(phenoxymethyl)azetidin-1-ylsulfonyl)indoline-2,3-dione
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C29H29FN2O7S
 1
1 IC50 = 27.9 nM
CP0291724
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C27H45N5O11
 1
1 IC50 = 29 nM
CP0109321
5-(2-(Pyridin-3-yl-oxymethyl)-pyrrolidine-1-sulfonyl)-1H-indole-2,3-dione
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C18H17N3O5S
 2
1 IC50 = 58.3 nM
2 IC50 = 58.88 nM
CP0074000
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3-methoxypyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C26H41N5O11
 1
1 IC50 = 59 nM
CP0041050
US10167313, Compound 53
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C31H38N4O11S
 1
1 IC50 = 90 nM
CP0136663
(S)-1-Methyl-5-(2-phenoxymethyl-azetidine-1-sulfonyl)-1H-indole-2,3-dione
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C19H18N2O5S
 2
1 IC50 = 91.2 nM
2 IC50 = 91.7 nM
CP0255351
(S)-5-(2-Phenoxymethyl-azetidine-1-sulfonyl)-1H-indole-2,3-dione
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C18H16N2O5S
 2
1 IC50 = 286.7 nM
2 IC50 = 288.4 nM
CP0282494
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[7-bromo-1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3,4-dihydro-1H-isoquinolin-2-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C30H40BrN5O10
 1
1 IC50 = 1075 nM
CP0333447
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-7-methyl-3,4-dihydro-1H-isoquinolin-2-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C31H43N5O10
 1
1 IC50 = 1410 nM
CP0227959
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3-(4-methylphenyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C32H45N5O10
 1
1 IC50 = 2765 nM
CP0062853
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-3-(2,2-dimethylpropyl)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C30H49N5O10
 1
1 IC50 = 2925 nM
CP0205131
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-6-methyl-3,4-dihydro-1H-isoquinolin-2-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C31H43N5O10
 1
1 IC50 = 3000 nM
CP0205130
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3R)-3-cyclohexyl-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C31H49N5O10
 1
1 IC50 = 4075 nM
CP0286834
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-3-butan-2-yloxy-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C29H47N5O11
 1
1 IC50 = 5125 nM
CP0233760
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3-propan-2-yloxypyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C28H45N5O11
 1
1 IC50 = 5533 nM
CP0302543
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C32H45N5O12
 1
1 IC50 = 7970 nM
CP0282492
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3-pyrimidin-2-yloxypyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C29H41N7O11
 1
1 IC50 = 9920 nM
CP0271657
(3S)-3-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-[[(2S)-1-[(2S,3S)-2-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]-3-propan-2-yloxypiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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C29H47N5O11
 1
1 IC50 = 81500 nM
CP0036823
(-)-etoposide
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C29H32O13
 1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( Caspase-3 (CASP3) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Anaplastic astrocytoma [ICD-11: 2A00.0]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PAC1 Phase 1
Anaplastic astrocytoma