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Target
Dual specificity mitogen-activated protein kinase kinase 2
Ligand
BDBM50382959
Substrate
n/a
Meas. Tech.
ChEMBL_817995 (CHEMBL2033421)
Kd
8300±n/a nM
Citation
Rowbottom, MW; Faraoni, R; Chao, Q; Campbell, BT; Lai, AG; Setti, E; Ezawa, M; Sprankle, KG; Abraham, S; Tran, L; Struss, B; Gibney, M; Armstrong, RC; Gunawardane, RN; Nepomuceno, RR; Valenta, I; Hua, H; Gardner, MF; Cramer, MD; Gitnick, D; Insko, DE; Apuy, JL; Jones-Bolin, S; Ghose, AK; Herbertz, T; Ator, MA; Dorsey, BD; Ruggeri, B; Williams, M; Bhagwat, S; James, J; Holladay, MW Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem 55:1082-105 (2012) [PubMed] Article
More Info.:
Target
Name:
Dual specificity mitogen-activated protein kinase kinase 2
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
Type:
Enzyme Catalytic Domain
Mol. Mass.:
44423.61
Organism:
Homo sapiens (Human)
Description:
gi_13489054
Residue:
400
Sequence:
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADLKMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV