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Target
Nicotinamide phosphoribosyltransferase
Ligand
BDBM217307
Substrate
n/a
Meas. Tech.
Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Binding Assay
pH
7.5±n/a
IC50
0.973±n/a nM
Comments
extracted
Citation
 Curtin, ML; Sorensen, BK; Heyman, HR; Clark, RF; Woller, KR; Shah, OJ; Michaelides, M; Tse, C; Vasudevan, A; Mack, H; Hansen, TM; Sweis, R; Pliushchev, MA NAMPT and rock inhibitors US Patent  US9302989 Publication Date 4/5/2016 
Target
Name:
Nicotinamide phosphoribosyltransferase
Synonyms:
NAMPT | NAMPT_HUMAN | NAmPRTase | Nicotinamide phosphoribosyltransferase | Nicotinamide phosphoribosyltransferase (NAMPT) | PBEF | PBEF1 | Pre-B-cell colony-enhancing factor 1
Type:
Enzyme
Mol. Mass.:
55524.98
Organism:
Homo sapiens (Human)
Description:
P43490
Residue:
491
Sequence:
MNPAAEAEFNILLATDSYKVTHYKQYPPNTSKVYSYFECREKKTENSKLRKVKYEETVFYGLQYILNKYLKGKVVTKEKIQEAKDVYKEHFQDDVFNEKGWNYILEKYDGHLPIEIKAVPEGFVIPRGNVLFTVENTDPECYWLTNWIETILVQSWYPITVATNSREQKKILAKYLLETSGNLDGLEYKLHDFGYRGVSSQETAGIGASAHLVNFKGTDTVAGLALIKKYYGTKDPVPGYSVPAAEHSTITAWGKDHEKDAFEHIVTQFSSVPVSVVSDSYDIYNACEKIWGEDLRHLIVSRSTQAPLIIRPDSGNPLDTVLKVLEILGKKFPVTENSKGYKLLPPYLRVIQGDGVDINTLQEIVEGMKQKMWSIENIAFGSGGGLLQKLTRDLLNCSFKCSYVVTNGLGINVFKDPVADPNKRSKKGRLSLHRTPAGNFVTLEEGKGDLEEYGQDLLHTVFKNGKVTKSYSFDEIRKNAQLNIELEAAHH
  
Inhibitor
Name:
BDBM217307
Synonyms:
US9302989, 1548
Type:
Small organic molecule
Emp. Form.:
C24H30N4O2
Mol. Mass.:
406.5206
SMILES:
CC(C)C(=O)N[C@H]1CC[C@H](CC1)c1ccc(NC(=O)N2Cc3ccncc3C2)cc1 |wU:6.5,9.12,(-8.88,-1.64,;-8.11,-.31,;-8.88,1.02,;-6.57,-.31,;-5.8,-1.64,;-5.8,1.02,;-4.26,1.02,;-3.49,2.36,;-1.95,2.36,;-1.18,1.02,;-1.95,-.31,;-3.49,-.31,;.36,1.02,;1.13,-.31,;2.67,-.31,;3.44,1.02,;4.98,1.02,;5.75,2.36,;4.98,3.69,;7.29,2.36,;8.2,3.6,;9.66,3.13,;10.99,3.9,;12.33,3.13,;12.33,1.59,;10.99,.82,;9.66,1.59,;8.2,1.11,;2.67,2.36,;1.13,2.36,)|
Structure:
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