Reaction Details
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Mitogen-activated protein kinase 1
Ligand
BDBM201751
Substrate
n/a
Meas. Tech.
IMAP-FP Assay
IC50
3.6±n/a nM
Citation
Wilson, KJ; Witter, DJ; Siliphaivanh, P; Lipford, K; Sloman, D; Falcone, D; O'Boyle, B; Mansoor, UF; Lim, J; Methot, JL; Boyce, C; Chen, L; Daniels, MH; Fevrier, S; Huang, X; Kurukulasuriya, R; Tong, L; Zhou, W; Kozlowski, J; Maletic, MM; Shinkre, BA; Thatai, JT; Bakshi, RK; Karunakaran, GB Compounds that are ERK inhibitors US Patent US9233979 Publication Date 1/12/2016 More Info.:
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:
Homo sapiens (Human)
Description:
P28482
Residue:
360
Sequence:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
Inhibitor
Name:
BDBM201751
Synonyms:
US9233979, 182 | US9233979, 183
Type:
Small organic molecule
Emp. Form.:
C24H32N6O3
Mol. Mass.:
452.5493
SMILES:
COC[C@@H](NC(=O)Nc1cc2[nH]nc(NCC3CC(C3)C(C)(C)O)c2cn1)c1ccccc1 |r,wU:3.3,(5.81,1.15,;4.48,.38,;3.14,1.15,;3.14,2.69,;1.81,3.46,;1.81,5,;3.14,5.77,;.48,5.77,;-.86,5,;-2.19,5.77,;-3.52,5,;-4.99,5.47,;-5.89,4.23,;-4.99,2.98,;-5.39,1.49,;-4.3,.4,;-4.7,-1.08,;-6.03,-1.85,;-5.26,-3.19,;-3.93,-2.42,;-5.66,-4.68,;-7.15,-5.07,;-4.17,-4.28,;-4.57,-5.77,;-3.52,3.46,;-2.19,2.69,;-.86,3.46,;4.48,3.46,;5.81,2.69,;7.15,3.46,;7.15,5,;5.81,5.77,;4.48,5,)|
Structure:
