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Target
Eukaryotic elongation factor 2 kinase
Ligand
BDBM138348
Substrate
n/a
Meas. Tech.
ChEMBL_1510608 (CHEMBL3607956)
IC50
>10000±n/a nM
Citation
 Papeo, G; Posteri, H; Borghi, D; Busel, AA; Caprera, F; Casale, E; Ciomei, M; Cirla, A; Corti, E; D'Anello, M; Fasolini, M; Forte, B; Galvani, A; Isacchi, A; Khvat, A; Krasavin, MY; Lupi, R; Orsini, P; Perego, R; Pesenti, E; Pezzetta, D; Rainoldi, S; Riccardi-Sirtori, F; Scolaro, A; Sola, F; Zuccotto, F; Felder, ER; Donati, D; Montagnoli, A Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. J Med Chem 58:6875-98 (2015) [PubMed]  Article 
Target
Name:
Eukaryotic elongation factor 2 kinase
Synonyms:
Calcium/calmodulin-dependent eukaryotic elongation factor 2 kinase | EEF2K | EF2K_HUMAN | Eukaryotic elongation factor 2 kinase (EEF2K) | Eukaryotic elongation factor 2 kinase (eEF-2K) | Serine/threonine-protein kinase EEF2K | eEF-2 kinase | eEF-2K
Type:
Protein
Mol. Mass.:
82116.99
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
725
Sequence:
MADEDLIFRLEGVDGGQSPRAGHDGDSDGDSDDEEGYFICPITDDPSSNQNVNSKVNKYYSNLTKSERYSSSGSPANSFHFKEAWKHAIQKAKHMPDPWAEFHLEDIATERATRHRYNAVTGEWLDDEVLIKMASQPFGRGAMRECFRTKKLSNFLHAQQWKGASNYVAKRYIEPVDRDVYFEDVRLQMEAKLWGEEYNRHKPPKQVDIMQMCIIELKDRPGKPLFHLEHYIEGKYIKYNSNSGFVRDDNIRLTPQAFSHFTFERSGHQLIVVDIQGVGDLYTDPQIHTETGTDFGDGNLGVRGMALFFYSHACNRICESMGLAPFDLSPRERDAVNQNTKLLQSAKTILRGTEEKCGSPQVRTLSGSRPPLLRPLSENSGDENMSDVTFDSLPSSPSSATPHSQKLDHLHWPVFSDLDNMASRDHDHLDNHRESENSGDSGYPSEKRGELDDPEPREHGHSYSNRKYESDEDSLGSSGRVCVEKWNLLNSSRLHLPRASAVALEVQRLNALDLEKKIGKSILGKVHLAMVRYHEGGRFCEKGEEWDQESAVFHLEHAANLGELEAIVGLGLMYSQLPHHILADVSLKETEENKTKGFDYLLKAAEAGDRQSMILVARAFDSGQNLSPDRCQDWLEALHWYNTALEMTDCDEGGEYDGMQDEPRYMMLAREAEMLFTGGYGLEKDPQRSGDLYTQAAEAAMEAMKGRLANQYYQKAEEAWAQMEE
  
Inhibitor
Name:
BDBM138348
Synonyms:
US8877944, 99
Type:
Small organic molecule
Emp. Form.:
C20H24F3N3O2
Mol. Mass.:
395.4187
SMILES:
NC(=O)c1cc(F)cc2CN(C3CCN(CC3)C3CCC(F)(F)CC3)C(=O)c12
Structure:
Search PDB for entries with ligand similarity: