Reaction Details |
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Target | MAP kinase-activated protein kinase 3 |
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Ligand | BDBM50242737 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_531386 (CHEMBL966741) |
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IC50 | >10000±n/a nM |
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Citation | McDermott, U; Sharma, SV; Dowell, L; Greninger, P; Montagut, C; Lamb, J; Archibald, H; Raudales, R; Tam, A; Lee, D; Rothenberg, SM; Supko, JG; Sordella, R; Ulkus, LE; Iafrate, AJ; Maheswaran, S; Njauw, CN; Tsao, H; Drew, L; Hanke, JH; Ma, XJ; Erlander, MG; Gray, NS; Haber, DA; Settleman, J Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A104:19936-41 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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MAP kinase-activated protein kinase 3 |
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Name: | MAP kinase-activated protein kinase 3 |
Synonyms: | 3pK | Chromosome 3p kinase | MAP kinase-activated protein kinase 3 (MAPKAP-K3) | MAPK-Activated Protein Kinase 3 (MK3) | MAPK-activated protein kinase 3 | MAPK3_HUMAN | MAPKAP kinase 3 | MAPKAPK-3 | MAPKAPK3 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 42991.57 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant MAPKAPK3 was phosphorylated by incubation with active p38alpha before assays. |
Residue: | 382 |
Sequence: | MDGETAEEQGGPVPPPVAPGGPGLGGAPGGRREPKKYAVTDDYQLSKQVLGLGVNGKVLE
CFHRRTGQKCALKLLYDSPKARQEVDHHWQASGGPHIVCILDVYENMHHGKRCLLIIMEC
MEGGELFSRIQERGDQAFTEREAAEIMRDIGTAIQFLHSHNIAHRDVKPENLLYTSKEKD
AVLKLTDFGFAKETTQNALQTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGFP
PFYSNTGQAISPGMKRRIRLGQYGFPNPEWSEVSEDAKQLIRLLLKTDPTERLTITQFMN
HPWINQSMVVPQTPLHTARVLQEDKDHWDEVKEEMTSALATMRVDYDQVKIKDLKTSNNR
LLNKRRKKQAGSSSASQGCNNQ
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BDBM50242737 |
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n/a |
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Name | BDBM50242737 |
Synonyms: | (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one | CHEMBL450786 | PHA-665752 | TCMDC-125885 |
Type | Small organic molecule |
Emp. Form. | C32H34Cl2N4O4S |
Mol. Mass. | 641.608 |
SMILES | Cc1[nH]c(\C=C2/C(=O)Nc3ccc(cc23)S(=O)(=O)Cc2c(Cl)cccc2Cl)c(C)c1C(=O)N1CCC[C@@H]1CN1CCCC1 |r| |
Structure |
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