General Information of the Protein
Protein ID
PT02896
Protein Name
Tryptophan 2,3-dioxygenase
Secondarily
Protein Name
Tryptamin 2,3-dioxygenase
Tryptophan oxygenase
Tryptophan pyrrolase
Tryptophanase
Gene Name
TDO2
Secondarily
Gene Name
TDO
Sequence
MSGCPFLGNNFGYTFKKLPVEGSEEDKSQTGVNRASKGGLIYGNYLHLEKVLNAQELQSETKGNKIHDEHLFIITHQAYELWFKQILWELDSVREIFQNGHVRDERNMLKVVSRMHRVSVILKLLVQQFSILETMTALDFNDFREYLSPASGFQSLQFRLLENKIGVLQNMRVPYNRRHYRDNFKGEENELLLKSEQEKTLLELVEAWLERTPGLEPHGFNFWGKLEKNITRGLEEEFIRIQAKEESEEKEEQVAEFQKQKEVLLSLFDEKRHEHLLSKGERRLSYRALQGALMIYFYREEPRFQVPFQLLTSLMDIDSLMTKWRYNHVCMVHRMLGSKAGTGGSSGYHYLRSTVSDRYKVFVDLFNLSTYLIPRHWIPKMNPTIHKFLYTAEYCDSSYFSSDESD
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Heme-dependent dioxygenase that catalyzes the oxidative cleavage of the L-tryptophan (L-Trp) pyrrole ring and converts L-tryptophan to N-formyl-L-kynurenine. Catalyzes the oxidative cleavage of the indole moiety.
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Uniprot ID
Primary ID:
P48775

Secondarily ID:
A8K053
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Ensembl ID
ENSG00000151790
HGNC ID
HGNC:11708
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: CL000438 , A-172
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0544887
 Compound Info 
2-[5-(6-fluoro-1H-indol-3-yl)-3-methyl-1,1-dioxo-3H-1,2-benzothiazol-2-yl]acetamide
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C18H16FN3O3S
  1
1
IC50 = 26 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0465020
 Compound Info 
(3R)-5-(6-fluoro-1H-indol-3-yl)-3-methyl-2,3-dihydro-1,2-benzothiazole 1,1-dioxide
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C16H13FN2O2S
  1
1
IC50 = 27 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0451811
 Compound Info 
[5-(6-fluoro-1H-indol-3-yl)-1,1-dioxo-2,3-dihydro-1,2-benzothiazol-3-yl]methanol
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C16H13FN2O3S
  1
1
IC50 = 43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0566878
 Compound Info 
4-[[5-(6-fluoro-1H-indol-3-yl)-3-methyl-1,1-dioxo-3H-1,2-benzothiazol-2-yl]methyl]-4-methyl-1,3-oxazolidin-2-one
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C21H20FN3O4S
  1
1
IC50 = 58 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0510722
 Compound Info 
3-[5-(6-fluoro-1H-indol-3-yl)-3-methyl-1,1-dioxo-3H-1,2-benzothiazol-2-yl]-N-methylpropanamide
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C20H20FN3O3S
  1
1
IC50 = 71 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0537584
 Compound Info 
2-[5-(6-fluoro-1H-indol-3-yl)-3-methyl-1,1-dioxo-3H-1,2-benzothiazol-2-yl]ethanesulfonamide
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C18H18FN3O4S2
  1
1
IC50 = 309 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000154 , HEK293-EBNA1-6E
 Cell Line Info 
Cell Line ID: CL000784 , P815B
 Cell Line Info 
Cell Line ID: CL000518 , SW48
 Cell Line Info 
Cell Line ID: CL000015 , SW480
 Cell Line Info 
Cell Line ID: CL000102 , U-87MG ATCC
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0073699
 Compound Info 
4-(4-fluoropyrazol-1-yl)-1,2-oxazol-5-amine
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C6H5FN4O
  2
1 EC50 = 77 nM
2 IC50 = 340 nM
CP0119011
 Compound Info 
(1R,4r)-4-((R)-2-((S)-6-fluoro-5H-imidazo[5,1- a]isoindol-5-yl)-1-hydroxyethyl)cyclohexanol
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C18H21FN2O2
  3
1 EC50 = 2000 nM
2 IC50 = 140 nM
3 IC50 = 800 nM
CP0355662
 Compound Info 
1-(3-chloro-4-fluorophenyl)-6-fluorobenzo[f]benzotriazole-4,9-dione
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C16H6ClF2N3O2
  1
1 IC50 = 4 nM
CP0234045
 Compound Info 
4-thiophen-3-yl-1,2-oxazol-5-amine
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C7H6N2OS
  1
1 IC50 = 28 nM
CP0346370
 Compound Info 
4-thiophen-2-yl-1,2-oxazol-5-amine
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C7H6N2OS
  1
1 IC50 = 29 nM
CP0569762
 Compound Info 
1-(chloromethyl)-6,6-dimethylnaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H13ClO4
  1
1 IC50 = 110 nM
CP0230210
 Compound Info 
(4S,5S)-5-[(5S)-5H-imidazo[5,1-a]isoindol-5-yl]-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-4-ol
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C17H16N4O
  1
1 IC50 = 130 nM
CP0080260
 Compound Info 
4-phenyl-1,2-oxazol-5-amine
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C9H8N2O
  1
1 IC50 = 140 nM
CP0571819
 Compound Info 
(6,6-dimethyl-7,10,11-trioxonaphtho[1,2-g][1]benzofuran-1-yl)methyl acetate
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C21H16O6
  2
1 IC50 = 160 nM
2 Ki = 730 nM
CP0364637
 Compound Info 
N-methyl-4-phenyl-1,2-oxazol-5-amine
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C10H10N2O
  1
1 IC50 = 190 nM
CP0578578
 Compound Info 
1-(hydroxymethyl)-6,6-dimethyl-8,9-dihydronaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H16O5
  1
1 IC50 = 200 nM
CP0469397
 Compound Info 
5-phenylthiadiazol-4-amine
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C8H7N3S
  1
1 IC50 = 270 nM
CP0070765
 Compound Info 
6-Fluoro-3-((E)-2-pyridin-3-yl-vinyl)-1H-indole
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C15H11FN2
  5
1 IC50 = 280 nM
2 IC50 = 350 nM
3 IC50 = 376.5 nM
4 IC50 = 937 nM
5 IC50 = 1300 nM
CP0080261
 Compound Info 
4-pyrazol-1-yl-1,2-oxazol-5-amine
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C6H6N4O
  1
1 IC50 = 290 nM
CP0579363
 Compound Info 
[(7S)-1,6,6-trimethyl-10,11-dioxo-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-7-yl] acetate
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C21H20O5
  1
1 IC50 = 370 nM
CP0350803
 Compound Info 
1-(hydroxymethyl)-6,6-dimethylnaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H14O5
  1
1 IC50 = 450 nM
CP0576804
 Compound Info 
PRZEWAQUINONE A
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C19H18O4
  1
1 IC50 = 450 nM
CP0225530
 Compound Info 
4-(3-chlorophenyl)-1,2-oxazol-5-amine
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C9H7ClN2O
  2
1 IC50 = 500 nM
2 IC50 = 2940 nM
CP0569395
 Compound Info 
1-(fluoromethyl)-6,6-dimethylnaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H13FO4
  1
1 IC50 = 570 nM
CP0222808
 Compound Info 
4-(4-fluorophenyl)-1,2-oxazol-5-amine
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C9H7FN2O
  1
1 IC50 = 580 nM
CP0072203
 Compound Info 
US10155972, Compound LM10
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C11H8FN5
  3
1 IC50 = 620 nM
2 IC50 = 2000 nM
3 Ki = 5500 nM
CP0080251
 Compound Info 
4-cyclopentyl-1,2-oxazol-5-amine
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C8H12N2O
  1
1 IC50 = 640 nM
CP0571820
 Compound Info 
(6,6-dimethyl-7,10,11-trioxo-8,9-dihydronaphtho[1,2-g][1]benzofuran-1-yl)methyl acetate
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C21H18O6
  1
1 IC50 = 670 nM
CP0578083
 Compound Info 
9-bromo-1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione
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C19H17BrO3
  1
1 IC50 = 710 nM
CP0159403
 Compound Info 
8-fluoro-2-[(4-methylpiperazin-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
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C21H19FN4O2
  1
1 IC50 = 760 nM
CP0431574
 Compound Info 
8-fluoro-2-(4-methylpiperazin-1-yl)indolo[2,1-b]quinazoline-6,12-dione
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C20H17FN4O2
  1
1 IC50 = 760 nM
CP0073693
 Compound Info 
4-(4-chlorophenyl)-1,2-oxazol-5-amine
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C9H7ClN2O
  2
1 IC50 = 830 nM
2 IC50 = 4210 nM
CP0075091
 Compound Info 
indolo[2,1-b]quinazoline-6,12-dione
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C15H8N2O2
  1
1 IC50 = 900 nM
CP0579187
 Compound Info 
1,6,6-trimethyl-8,9-dihydronaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H16O4
  1
1 IC50 = 940 nM
CP0579362
 Compound Info 
1,6,6-trimethylnaphtho[1,2-g][1]benzofuran-7,10,11-trione
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C19H14O4
  1
1 IC50 = 960 nM
CP0569394
 Compound Info 
8-hydroxy-1,6,6-trimethylnaphtho[1,2-g][1]benzofuran-9,10,11-trione
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C19H14O5
  1
1 IC50 = 1010 nM
CP0579210
 Compound Info 
(7S)-7-hydroxy-1-(hydroxymethyl)-6,6-dimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione
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C19H18O5
  1
1 IC50 = 1010 nM
CP0578579
 Compound Info 
[(7S)-1,6,6-trimethyl-10,11-dioxo-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-7-yl] methanesulfonate
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C20H20O6S
  1
1 IC50 = 1210 nM
CP0579211
 Compound Info 
8-hydroxy-1,6,6-trimethyl-7,8-dihydronaphtho[1,2-g][1]benzofuran-9,10,11-trione
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C19H16O5
  1
1 IC50 = 1480 nM
CP0080253
 Compound Info 
4-(3-methylpyrazol-1-yl)-1,2-oxazol-5-amine
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C7H8N4O
  1
1 IC50 = 1600 nM
CP0559942
 Compound Info 
4-(4-methylpyrazol-1-yl)-1,2-oxazol-5-amine
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C7H8N4O
  1
1 IC50 = 1600 nM
CP0534912
 Compound Info 
4-pyridin-2-yl-1,2-oxazol-5-amine
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C8H7N3O
  1
1 IC50 = 1700 nM
CP0576805
 Compound Info 
[(7S)-1-(hydroxymethyl)-6,6-dimethyl-10,11-dioxo-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-7-yl] acetate
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C21H20O6
  1
1 IC50 = 1840 nM
CP0521484
 Compound Info 
4-pyridin-3-yl-1,2-oxazol-5-amine
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C8H7N3O
  1
1 IC50 = 2300 nM
CP0550329
 Compound Info 
[(7S)-7-hydroxy-6,6-dimethyl-10,11-dioxo-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-1-yl]methyl acetate
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C21H20O6
  1
1 IC50 = 2420 nM
CP0545404
 Compound Info 
3-Hydroxytanshinone
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C19H18O4
  1
1 IC50 = 2700 nM
CP0429359
 Compound Info 
4-(3-methoxyphenyl)-1,2-oxazol-5-amine
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C10H10N2O2
  1
1 IC50 = 3100 nM
CP0466617
 Compound Info 
(4-phenyl-1,2-oxazol-5-yl)methanol
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C10H9NO2
  1
1 IC50 = 4400 nM
CP0230444
 Compound Info 
4-cyclohexyl-1,2-oxazol-5-amine
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C9H14N2O
  1
1 IC50 = 7800 nM
CP0569181
 Compound Info 
N,N-diethyl-6,6-dimethyl-7,10,11-trioxonaphtho[1,2-g][1]benzofuran-1-carboxamide
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C23H21NO5
  1
1 IC50 = 9540 nM
CP0081974
 Compound Info 
US10034864, Example 1
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C11H13BrFN7O4S
  2
1 IC50 = 16100 nM
2 IC50 > 10000 nM
CP0222812
 Compound Info 
4-phenyl-1,2-thiazol-5-amine
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C9H8N2S
  1
1 IC50 = 18000 nM
CP0210888
 Compound Info 
3-methyl-4-phenyl-1,2-oxazol-5-amine
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C10H10N2O
  1
1 IC50 = 25000 nM
CP0165127
 Compound Info 
CHEMBL4161733
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C24H24ClFN2O
  2
1 IC50 > 2000 nM
2 IC50 > 10000 nM
CP0578577
 Compound Info 
6,6-dimethyl-7,10,11-trioxonaphtho[1,2-g][1]benzofuran-1-carboxylic acid
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C19H12O6
  1
1 IC50 > 10000 nM
CP0210992
 Compound Info 
2-methyl-4-phenylpyrazol-3-amine
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C10H11N3
  1
1 IC50 > 25000 nM
CP0248178
 Compound Info 
5-phenyl-1,2-oxazol-4-amine
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C9H8N2O
  1
1 IC50 > 25000 nM
CP0248179
 Compound Info 
3-phenyltriazol-4-amine
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C8H8N4
  1
1 IC50 > 25000 nM
CP0346369
 Compound Info 
4-phenyl-1,2-oxazole
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C9H7NO
  1
1 IC50 > 25000 nM
CP0354580
 Compound Info 
4-phenyl-1,2-oxazole-5-carboxamide
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C10H8N2O2
  1
1 IC50 > 25000 nM
CP0354582
 Compound Info 
4-phenyl-1H-pyrazol-5-amine
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C9H9N3
  1
1 IC50 > 25000 nM
CP0364638
 Compound Info 
4-phenyl-1,2,4-triazol-3-amine
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C8H8N4
  1
1 IC50 > 25000 nM
CP0473820
 Compound Info 
4-phenylthiadiazol-5-amine
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C8H7N3S
  1
1 IC50 > 25000 nM
CP0534913
 Compound Info 
5-phenyl-1,2-thiazol-4-amine
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C9H8N2S
  1
1 IC50 > 25000 nM
CP0543217
 Compound Info 
N-methyl-4-phenyl-1,2-oxazole-5-carboxamide
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C11H10N2O2
  1
1 IC50 > 25000 nM
Clinical Information about the Protein
Target 1 ( Tryptophan 2,3-dioxygenase (TDO) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Preclinical Drug(s) 3 Preclinical Drugs  3
1 4-(4-fluoropyrazol-1-yl)-1,2-oxazol-5-amine
 Drug Info 
Preclinical
Solid tumour/cancer
2 680C91
 Drug Info 
Preclinical
Solid tumour/cancer
3 LM10
 Drug Info 
Preclinical
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT05447 Tryptophan 2,3-dioxygenase Mus musculus, Mouse
 Protein Info