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Target
Mitogen-activated protein kinase kinase kinase kinase 3
Ligand
BDBM50510309
Substrate
n/a
Meas. Tech.
ChEMBL_2020700 (CHEMBL4674513)
IC50
24±n/a nM
Citation
 May-Dracka, TL; Arduini, R; Bertolotti-Ciarlet, A; Bhisetti, G; Brickelmaier, M; Cahir-McFarland, E; Enyedy, I; Fontenot, JD; Hesson, T; Little, K; Lyssikatos, J; Marcotte, D; McKee, T; Murugan, P; Patterson, T; Peng, H; Rushe, M; Silvian, L; Spilker, K; Wu, P; Xin, Z; Burkly, LC Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKC? phosphorylation: Potential therapy to modulate T cell dependent immunity. Bioorg Med Chem Lett 28:1964-1971 (2018) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 3
Synonyms:
M4K3_HUMAN | MAP4K3 | RAB8IPL1
Type:
PROTEIN
Mol. Mass.:
101331.91
Organism:
Homo sapiens (Human)
Description:
ChEMBL_586461
Residue:
894
Sequence:
MNPGFDLSRRNPQEDFELIQRIGSGTYGDVYKARNVNTGELAAIKVIKLEPGEDFAVVQQEIIMMKDCKHPNIVAYFGSYLRRDKLWICMEFCGGGSLQDIYHVTGPLSELQIAYVSRETLQGLYYLHSKGKMHRDIKGANILLTDNGHVKLADFGVSAQITATIAKRKSFIGTPYWMAPEVAAVERKGGYNQLCDLWAVGITAIELAELQPPMFDLHPMRALFLMTKSNFQPPKLKDKMKWSNSFHHFVKMALTKNPKKRPTAEKLLQHPFVTQHLTRSLAIELLDKVNNPDHSTYHDFDDDDPEPLVAVPHRIHSTSRNVREEKTRSEITFGQVKFDPPLRKETEPHHELPDSDGFLDSSEEIYYTARSNLDLQLEYGQGHQGGYFLGANKSLLKSVEEELHQRGHVAHLEDDEGDDDESKHSTLKAKIPPPLPPKPKSIFIPQEMHSTEDENQGTIKRCPMSGSPAKPSQVPPRPPPPRLPPHKPVALGNGMSSFQLNGERDGSLCQQQNEHRGTNLSRKEKKDVPKPISNGLPPTPKVHMGACFSKVFNGCPLKIHCASSWINPDTRDQYLIFGAEEGIYTLNLNELHETSMEQLFPRRCTWLYVMNNCLLSISGKASQLYSHNLPGLFDYARQMQKLPVAIPAHKLPDRILPRKFSVSAKIPETKWCQKCCVVRNPYTGHKYLCGALQTSIVLLEWVEPMQKFMLIKHIDFPIPCPLRMFEMLVVPEQEYPLVCVGVSRGRDFNQVVRFETVNPNSTSSWFTESDTPQTNVTHVTQLERDTILVCLDCCIKIVNLQGRLKSSRKLSSELTFDFQIESIVCLQDSVLAFWKHGMQGRSFRSNEVTQEISDSTRIFRLLGSDRVVVLESRPTDNPTANSNLYILAGHENSY
  
Inhibitor
Name:
BDBM50510309
Synonyms:
CHEMBL4568440
Type:
Small organic molecule
Emp. Form.:
C22H24Cl2FN5O
Mol. Mass.:
464.363
SMILES:
CCC(Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl
Structure:
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