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Target
Mitogen-activated protein kinase 1
Ligand
BDBM35663
Substrate
erktide
Meas. Tech.
Ki Determination
pH
7.5±n/a
Temperature
303.15±n/a K
Ki
<2±n/a nM
Citation
Aronov, AM; Tang, Q; Martinez-Botella, G; Bemis, GW; Cao, J; Chen, G; Ewing, NP; Ford, PJ; Germann, UA; Green, J; Hale, MR; Jacobs, M; Janetka, JW; Maltais, F; Markland, W; Namchuk, MN; Nanthakumar, S; Poondru, S; Straub, J; ter Haar, E; Xie, X Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. J Med Chem 52:6362-8 (2009) [PubMed] Article
Target
Name:
Mitogen-activated protein kinase 1
Synonyms:
ERK2 | ERT1 | Extracellular signal-regulated kinase 2 | Extracellular signal-regulated kinase 2 (ERK-2) | Extracellular signal-regulated kinase 2 (ERK2) | MAP Kinase 2/ERK2 | MAPK 2 | MAPK1 | MK01_HUMAN | Mitogen activated kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK2) | Mitogen-activated protein kinase 2 | PRKM1 | PRKM2 | p42-MAPK
Type:
Ser/Thr Protein Kinase
Mol. Mass.:
41392.76
Organism:
Human
Description:
P28482
Residue:
360
Sequence:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
Inhibitor
Name:
BDBM35663
Synonyms:
pyrimidylpyrrole, 11k
Type:
Small organic molecule
Emp. Form.:
C25H20ClF2N5O4
Mol. Mass.:
527.907
SMILES:
Cc1cnc(Nc2cccc3OC(F)(F)Oc23)nc1-c1c[nH]c(c1)C(=O)N[C@H](CO)c1cccc(Cl)c1 |r|
Substrate
Name:
ERKtide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1314.49
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
ATGPLSPGPFGRR