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Literature summary for 1.13.11.52 extracted from

  • Li, Y.; Zhang, S.; Wang, R.; Cui, M.; Liu, W.; Yang, Q.; Kuang, C.
    Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase (2020), Bioorg. Med. Chem. Lett., 30, 127159 .
    View publication on PubMed
Search for more literature for 1.13.11.52

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoic acid
-
 Homo sapiens
(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)boronic acid
-
 Homo sapiens
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylic acid
-
 Homo sapiens
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]proline
-
 Homo sapiens
8-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolo[2,1-b]quinazoline-6,12-dione
-
 Homo sapiens
8-fluoro-2-[(1H-1,2,3-triazol-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
-
 Homo sapiens
8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbaldehyde
-
 Homo sapiens
8-fluorotryptanthrin
-
 Homo sapiens
epacadostat INCB024360 Homo sapiens
ethyl (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoate
-
 Homo sapiens
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylate
-
 Homo sapiens
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylate
-
 Homo sapiens
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]prolinate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14902
-
-

Synonyms

Synonyms Comment Organism
IDO1
-
 Homo sapiens
indoleamine 2,3-dioxygenase 1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00009
-
 pH and temperature not specified in the publication Homo sapiens epacadostat
0.00012
-
 pH and temperature not specified in the publication Homo sapiens (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoic acid
0.00019
-
 pH and temperature not specified in the publication Homo sapiens ethyl (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoate
0.00046
-
 pH and temperature not specified in the publication Homo sapiens 8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbaldehyde
0.00046
-
 pH and temperature not specified in the publication Homo sapiens methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]prolinate
0.00048
-
 pH and temperature not specified in the publication Homo sapiens 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylic acid
0.000534
-
 pH and temperature not specified in the publication Homo sapiens 8-fluorotryptanthrin
0.00055
-
 pH and temperature not specified in the publication Homo sapiens 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]proline
0.00057
-
 pH and temperature not specified in the publication Homo sapiens 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylic acid
0.00078
-
 pH and temperature not specified in the publication Homo sapiens 8-fluoro-2-[(1H-1,2,3-triazol-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
0.0012
-
 pH and temperature not specified in the publication Homo sapiens methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylate
0.00143
-
 pH and temperature not specified in the publication Homo sapiens methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylate
0.00179
-
 pH and temperature not specified in the publication Homo sapiens (8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)boronic acid
0.01309
-
 pH and temperature not specified in the publication Homo sapiens 8-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolo[2,1-b]quinazoline-6,12-dione

General Information

General Information Comment Organism
drug target Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are promising drug development targets due to their implications in pathologies such as cancer and neurodegenerative diseases. IDO1/TDO dual inhibitors and provides chemical molecules for potential development into drugs Homo sapiens
physiological function the enzyme is overactivated or overexpressed in many human cancers, which is associated with poor patient outcomes Homo sapiens