| Reaction Details |
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 | Report a problem with these data |
| Target | Dual specificity mitogen-activated protein kinase kinase 1/2 |
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| Ligand | BDBM26198 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_60727 (CHEMBL671987) |
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| IC50 | 160±n/a nM |
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| Citation |  Thompson, JE; Cubbon, RM; Cummings, RT; Wicker, LS; Frankshun, R; Cunningham, BR; Cameron, PM; Meinke, PT; Liverton, N; Weng, Y; DeMartino, JA Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett12:1219-23 (2002) [PubMed] |
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| More Info.: | Get all data from this article, Assay Method |
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| Dual specificity mitogen-activated protein kinase kinase 1/2 |
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| Name: | Dual specificity mitogen-activated protein kinase kinase 1/2 |
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| Synonyms: | Dual specificity mitogen-activated protein kinase kinase; MEK1/2 | p-MEK1/2 |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 795758 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Dual specificity mitogen-activated protein kinase kinase 2 |
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| Synonyms: | Dual specificity mitogen-activated protein kinase kinase 2 (MEK2) | Dual specificity mitogen-activated protein kinase kinase; MEK1/2 | ERK activator kinase 2 | MAP kinase kinase 2 | MAP2K2 | MAPK/ERK kinase 2 | MAPKK 2 | MEK2 | MKK2 | MP2K2_HUMAN | PRKMK2 | VHL-MAP2K1/MAP2K2 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 44423.61 |
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| Organism: | Homo sapiens (Human) |
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| Description: | gi_13489054 |
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| Residue: | 400 |
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| Sequence: | MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV
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| Component 2 |
| Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Synonyms: | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2 |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 43439.03 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates. |
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| Residue: | 393 |
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| Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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| BDBM26198 |
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| n/a |
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| Name | BDBM26198 |
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| Synonyms: | 4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11.4.0.0^{2,6}.0^{7,12}]heptadeca-1(13),2(6),3,7(12),8,14,16-heptaen-11-one | CHEMBL21156 | Compound # 2 | Jak Inhibitor 1 | PDK1 inhibitor, 1 | Tetracyclic Pyridone, 1 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H16FN3O |
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| Mol. Mass. | 309.3375 |
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| SMILES | CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O |
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| Structure | 
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