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Target
Dual specificity mitogen-activated protein kinase kinase 5
Ligand
BDBM50434072
Substrate
n/a
Meas. Tech.
ChEMBL_1864566 (CHEMBL4365541)
IC50
1.5±n/a nM
Citation
 Myers, SM; Miller, DC; Molyneux, L; Arasta, M; Bawn, RH; Blackburn, TJ; Cook, SJ; Edwards, N; Endicott, JA; Golding, BT; Griffin, RJ; Hammonds, T; Hardcastle, IR; Harnor, SJ; Heptinstall, AB; Lochhead, PA; Martin, MP; Martin, NC; Newell, DR; Owen, PJ; Pang, LC; Reuillon, T; Rigoreau, LJM; Thomas, HD; Tucker, JA; Wang, LZ; Wong, AC; Noble, MEM; Wedge, SR; Cano, C Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38? and BRD4. Eur J Med Chem 178:530-543 (2019) [PubMed]  Article 
Target
Name:
Dual specificity mitogen-activated protein kinase kinase 5
Synonyms:
MAP kinase kinase 5 | MAP2K5 | MAPK/ERK kinase 5 | MAPKK 5 | MEK5 | MKK5 | MP2K5_HUMAN | PRKMK5
Type:
PROTEIN
Mol. Mass.:
50110.16
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1495740
Residue:
448
Sequence:
MLWLALGPFPAMENQVLVIRIKIPNSGAVDWTVHSGPQLLFRDVLDVIGQVLPEATTTAFEYEDEDGDRITVRSDEEMKAMLSYYYSTVMEQQVNGQLIEPLQIFPRACKPPGERNIHGLKVNTRAGPSQHSSPAVSDSLPSNSLKKSSAELKKILANGQMNEQDIRYRDTLGHGNGGTVYKAYHVPSGKILAVKVILLDITLELQKQIMSELEILYKCDSSYIIGFYGAFFVENRISICTEFMDGGSLDVYRKMPEHVLGRIAVAVVKGLTYLWSLKILHRDVKPSNMLVNTRGQVKLCDFGVSTQLVNSIAKTYVGTNAYMAPERISGEQYGIHSDVWSLGISFMELALGRFPYPQIQKNQGSLMPLQLLQCIVDEDSPVLPVGEFSEPFVHFITQCMRKQPKERPAPEELMGHPFIVQFNDGNAAVVSMWVCRALEERRSQQGPP
  
Inhibitor
Name:
BDBM50434072
Synonyms:
CHEMBL2381342
Type:
Small organic molecule
Emp. Form.:
C27H28N4O2
Mol. Mass.:
440.5368
SMILES:
CN(C)Cc1cccc(c1)N=C(C1C(=O)Nc2cc(ccc12)C(=O)N(C)C)c1ccccc1 |w:10.10|
Structure:
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