Target
Dual specificity mitogen-activated protein kinase kinase 4
Ligand
BDBM558858
Substrate
Mitogen-activated protein kinase 8
Meas. Tech.
ADP-Glo Kinase Activity Assay
IC50
240±n/a nM
Citation
 Scheidt, KASchiltz, GEClutter, MRKwong, AJ 3-arylindazoles as selective MEK4 inhibitors US Patent  US11370770 Publication Date 6/28/2022 
Target
Name:
Dual specificity mitogen-activated protein kinase kinase 4
Synonyms:
JNK-activating kinase 1 | JNKK | JNKK1 | MAP kinase kinase 4 | MAP2K4 | MEK4 | MKK4 | MP2K4_HUMAN | PRKMK4 | SAPK/ERK kinase 1 | SEK1 | SERK1 | SKK1 | c-Jun N-terminal kinase kinase 1
Type:
PROTEIN
Mol. Mass.:
44294.29
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1460558
Residue:
399
Sequence:
MAAPSPSGGGGSGGGSGSGTPGPVGSPAPGHPAVSSMQGKRKALKLNFANPPFKSTARFTLNPNPTGVQNPHIERLRTHSIESSGKLKISPEQHWDFTAEDLKDLGEIGRGAYGSVNKMVHKPSGQIMAVKRIRSTVDEKEQKQLLMDLDVVMRSSDCPYIVQFYGALFREGDCWICMELMSTSFDKFYKYVYSVLDDVIPEEILGKITLATVKALNHLKENLKIIHRDIKPSNILLDRSGNIKLCDFGISGQLVDSIAKTRDAGCRPYMAPERIDPSASRQGYDVRSDVWSLGITLYELATGRFPYPKWNSVFDQLTQVVKGDPPQLSNSEEREFSPSFINFVNLCLTKDESKRPKYKELLKHPFILMYEERAVEVACYVCKILDQMPATPSSPMYVD
  
Inhibitor
Name:
BDBM558858
Synonyms:
US11370770, Compound 6j
Type:
Small organic molecule
Emp. Form.:
C14H9F3N2O
Mol. Mass.:
278.2293
SMILES:
Oc1ccc(cc1)-c1n[nH]c2ccc(cc12)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Mitogen-activated protein kinase 8
Synonyms:
JNK-46 | JNK1 | JNK1-alpha-1 | MAPK8 | MK08_HUMAN | Mitogen-Activated Protein Kinase 8 (JNK1) | PRKM8 | SAPK1 | SAPK1C | Stress-activated protein kinase JNK1 | c-Jun N-terminal kinase 1 | c-Jun N-terminal kinase 1 (JNK1) | c-Jun N-terminal kinase 1(JNK1) | c-Jun N-terminal kinase 2 (JNK2)
Type:
Enzyme
Mol. Mass.:
48297.57
Organism:
Homo sapiens (Human)
Description:
JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology).
Residue:
427
Sequence:
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR