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Target
Mitogen-activated protein kinase 1
Ligand
BDBM272538
Substrate
n/a
Meas. Tech.
IMAP-FP assay
IC50
0.300±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 US9745307 Publication Date 8/29/2017
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:
BDBM272538
Synonyms:
3-(1-methyl-1H-pyrazol-4-yl)-1,8-dihydro-7H-pyrazolo[4,3-g]quinolin-7-one | US10065967, Example 4 | US10759805, Ex 4 | US9745307, Example 4
Type:
Small organic molecule
Emp. Form.:
C14H11N5O
Mol. Mass.:
265.27
SMILES:
Cn1cc(cn1)-c1n[nH]c2cc3[nH]c(=O)ccc3cc12