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Literature summary for 2.4.2.12 extracted from

  • Asawa, Y.; Katsuragi, K.; Sato, A.; Yoshimori, A.; Tanuma, S.I.; Nakamura, H.
    Structure-based drug design of novel carborane-containing nicotinamide phosphoribosyltransferase inhibitors (2019), Bioorg. Med. Chem., 27, 2832-2844 .
    View publication on PubMed
Search for more literature for 2.4.2.12

Inhibitors

Inhibitors Comment Organism Structure
(3R,5R,7R)-N-(4-((E)-3-(pyridin-3-yl)acrylamido)butyl)adamantane-1-carboxamide
-
 Homo sapiens
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidepentyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(1,7-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(1-(1,12-dicarba-closo-dodecaboranyl)piperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(1-benzoyl-1,12-dicarba-closo-dodecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(1-trimethylsilyl-1,12-dicarba-closododecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,7-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranyl(hydroxy)methyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
(E)-N-(4-(4-(1,7-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
 Homo sapiens
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,12-dicarba-closo-dodecaborane
-
 Homo sapiens
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
1-((E)-4-(3-(pyridin-3-yl)acrylamido)pentyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)butyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)pentyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)butyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)pentyl)-1,2-dicarba-closo-dodecaborane
-
 Homo sapiens
FK866
-
 Homo sapiens
tert-butyl ((1,12-dicarba-closo-dodecaboranylamido)propyl)carbamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
nicotinamide D-ribonucleotide + diphosphate Homo sapiens
-
 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P43490
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
MDA-MB-468 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
nicotinamide D-ribonucleotide + diphosphate
-
 Homo sapiens nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
Nampt
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000057
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
0.000098
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1,7-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
0.00017
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidepentyl)-3-(pyridin-3-yl)acrylamide
0.00018
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1-trimethylsilyl-1,12-dicarba-closododecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
0.00025
-
 at 30°C, pH not specified in the publication Homo sapiens 1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,12-dicarba-closo-dodecaborane
0.00032
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1-(1,12-dicarba-closo-dodecaboranyl)piperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
0.00037
-
 at 30°C, pH not specified in the publication Homo sapiens 1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,2-dicarba-closo-dodecaborane
0.00062
-
 at 30°C, pH not specified in the publication Homo sapiens FK866
0.00063
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(1-benzoyl-1,12-dicarba-closo-dodecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
0.00292
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,7-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
0.00376
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(4-(1,7-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
0.00451
-
 at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranyl(hydroxy)methyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
0.0049
-
 at 30°C, pH not specified in the publication Homo sapiens 1-((E)-4-(3-(pyridin-3-yl)acrylamido)pentyl)-1,2-dicarba-closo-dodecaborane
0.008
-
 at 30°C, pH not specified in the publication Homo sapiens (3R,5R,7R)-N-(4-((E)-3-(pyridin-3-yl)acrylamido)butyl)adamantane-1-carboxamide
0.01
-
 IC50 above 0.01 mM, at 30°C, pH not specified in the publication Homo sapiens (E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
0.03
-
 IC50 above 0.03 mM, at 30°C, pH not specified in the publication Homo sapiens 1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)butyl)-1,2-dicarba-closo-dodecaborane
0.03
-
 IC50 above 0.03 mM, at 30°C, pH not specified in the publication Homo sapiens 1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)pentyl)-1,2-dicarba-closo-dodecaborane
0.03
-
 IC50 above 0.03 mM, at 30°C, pH not specified in the publication Homo sapiens 1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)butyl)-1,2-dicarba-closo-dodecaborane
0.03
-
 IC50 above 0.03 mM, at 30°C, pH not specified in the publication Homo sapiens 1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)pentyl)-1,2-dicarba-closo-dodecaborane
0.03
-
 IC50 above 0.03 mM, at 30°C, pH not specified in the publication Homo sapiens tert-butyl ((1,12-dicarba-closo-dodecaboranylamido)propyl)carbamate