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Target
Dual specificity mitogen-activated protein kinase kinase 2
Ligand
BDBM4814
Substrate
n/a
Meas. Tech.
ChEMBL_586335 (CHEMBL1061079)
Kd
110±n/a nM
Citation
Karaman, MW; Herrgard, S; Treiber, DK; Gallant, P; Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Hunt, JP; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Wodicka, LM; Zarrinkar, PP A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol 26:127-32 (2008) [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
Inhibitor
Name:
BDBM4814
Synonyms:
CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide | SU11248 | SUNITINIB | SUNITINIB MALATE | US10464902, Sunitinib | US9163010, Sunitinib | US9914707, SU11248
Type:
Small organic molecule
Emp. Form.:
C22H27FN4O2
Mol. Mass.:
398.4738
SMILES:
CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C