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Target
Dual specificity mitogen-activated protein kinase kinase 2
Ligand
BDBM13216
Substrate
n/a
Meas. Tech.
ChEMBL_586335 (CHEMBL1061079)
Kd
1400±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:
BDBM13216
Synonyms:
BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide | N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide | US10294227, Code Dasatinib | US20230348453, Compound A8 | cid_3062316 | med.21724, Compound Dasatinib
Type:
Small organic molecule
Emp. Form.:
C22H26ClN7O2S
Mol. Mass.:
488.006
SMILES:
Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1