| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase kinase kinase kinase 3 |
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| Ligand | BDBM50306682 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2020700 (CHEMBL4674513) |
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| IC50 | 49±n/a nM |
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| 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 Lett28:1964-1971 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Mitogen-activated protein kinase kinase kinase kinase 3 |
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| Name: | Mitogen-activated protein kinase kinase kinase kinase 3 |
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| Synonyms: | M4K3_HUMAN | MAP4K3 | RAB8IPL1 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 101331.91 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_586461 |
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| Residue: | 894 |
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| Sequence: | MNPGFDLSRRNPQEDFELIQRIGSGTYGDVYKARNVNTGELAAIKVIKLEPGEDFAVVQQ
EIIMMKDCKHPNIVAYFGSYLRRDKLWICMEFCGGGSLQDIYHVTGPLSELQIAYVSRET
LQGLYYLHSKGKMHRDIKGANILLTDNGHVKLADFGVSAQITATIAKRKSFIGTPYWMAP
EVAAVERKGGYNQLCDLWAVGITAIELAELQPPMFDLHPMRALFLMTKSNFQPPKLKDKM
KWSNSFHHFVKMALTKNPKKRPTAEKLLQHPFVTQHLTRSLAIELLDKVNNPDHSTYHDF
DDDDPEPLVAVPHRIHSTSRNVREEKTRSEITFGQVKFDPPLRKETEPHHELPDSDGFLD
SSEEIYYTARSNLDLQLEYGQGHQGGYFLGANKSLLKSVEEELHQRGHVAHLEDDEGDDD
ESKHSTLKAKIPPPLPPKPKSIFIPQEMHSTEDENQGTIKRCPMSGSPAKPSQVPPRPPP
PRLPPHKPVALGNGMSSFQLNGERDGSLCQQQNEHRGTNLSRKEKKDVPKPISNGLPPTP
KVHMGACFSKVFNGCPLKIHCASSWINPDTRDQYLIFGAEEGIYTLNLNELHETSMEQLF
PRRCTWLYVMNNCLLSISGKASQLYSHNLPGLFDYARQMQKLPVAIPAHKLPDRILPRKF
SVSAKIPETKWCQKCCVVRNPYTGHKYLCGALQTSIVLLEWVEPMQKFMLIKHIDFPIPC
PLRMFEMLVVPEQEYPLVCVGVSRGRDFNQVVRFETVNPNSTSSWFTESDTPQTNVTHVT
QLERDTILVCLDCCIKIVNLQGRLKSSRKLSSELTFDFQIESIVCLQDSVLAFWKHGMQG
RSFRSNEVTQEISDSTRIFRLLGSDRVVVLESRPTDNPTANSNLYILAGHENSY
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| BDBM50306682 |
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| n/a |
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| Name | BDBM50306682 |
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| Synonyms: | (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine | 3-(2,6-dichloro-3-fluorobenzyloxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine | 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-amine | CHEMBL601719 | CRIZOTINIB | PF-2341066 | US10370379, Crizotinib | US10543199, Compound Crizotinib | US10780082, Compound Crizotinib | US11059827, Compound Crizotinib | US11517561, Compound Crizotinib | US9126941, PF-2341066 | US9199944, Crizotinib | US9226923, Crizotinib |
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| Type | Small organic molecule |
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| Emp. Form. | C21H22Cl2FN5O |
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| Mol. Mass. | 450.337 |
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| SMILES | C[C@@H](Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl |r| |
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| Structure | 
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