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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50604141
Substrate
n/a
Meas. Tech.
ChEMBL_2247058 (CHEMBL5161268)
IC50
1860±n/a nM
Citation
 Luo, G; Chen, L; Kostich, WA; Hamman, B; Allen, J; Easton, A; Bourin, C; Gulianello, M; Lippy, J; Nara, S; Pattipati, SN; Dandapani, K; Dokania, M; Vattikundala, P; Sharma, V; Elavazhagan, S; Verma, MK; Lal Das, M; Wagh, S; Balakrishnan, A; Johnson, BM; Santone, KS; Thalody, G; Denton, R; Saminathan, H; Holenarsipur, VK; Kumar, A; Rao, A; Putlur, SP; Sarvasiddhi, SK; Shankar, G; Louis, JV; Ramarao, M; Conway, CM; Li, YW; Pieschl, R; Tian, Y; Hong, Y; Bristow, L; Albright, CF; Bronson, JJ; Macor, JE; Dzierba, CD Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain. J Med Chem 65:4534-4564 (2022) [PubMed] 
Target
Name:
Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:
ERK activator kinase 1 | Mitogen-activated protein kinase 1 (MEK1) | MAPK/ERK kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | MEK-1 | MAP kinase kinase 1 | MAPK/ERK kinase 1 | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | MP2K1_HUMAN | MAP2K1 | MEK1 | PRKMK1 | VHL-MAP2K1/MAP2K2 | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase
Type:
Other Protein Type
Mol. Mass.:
43439.03
Organism:
Human
Description:
Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates.
Residue:
393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
  
Inhibitor
Name:
BDBM50604141
Synonyms:
CHEMBL5188433
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
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