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Target
Mitogen-activated protein kinase 1
Ligand
BDBM272545
Substrate
n/a
Meas. Tech.
Active Human ERK2 (hERK2) Activity Assay
IC50
459±n/a nM
Citation
Lim, J; Huang, X; Ferguson, RD; Zhou, W; Boyce, CW; Siliphaivanh, P; Witter, DJ; Maletic, MM; Kozlowski, JA; Wilson, KJ Compounds that are ERK inhibitors US Patent US10065967 Publication Date 9/4/2018
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:
BDBM272545
Synonyms:
7-(4-fluorobenzyl)-9-hydroxy-3-(2-methylpyridin-4-yl)-5,6,7,9-tetrahydro-[1,3]diazepino[5,4-f]indazol-8(1H)-one | US10065967, Example 11 | US9745307, Example 11
Type:
Small organic molecule
Emp. Form.:
C23H20FN5O2
Mol. Mass.:
417.4356
SMILES:
Cc1cc(ccn1)-c1n[nH]c2cc3N(O)C(=O)N(Cc4ccc(F)cc4)CCc3cc12