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Target
Mitogen-activated protein kinase 8
Ligand
BDBM27802
Substrate
Biotin-GST-c-JUN
Meas. Tech.
IGF-1R Inhibition Assay
IC50
1000±n/a nM
Citation
 Chamberlain, SD; Redman, AM; Wilson, JW; Deanda, F; Shotwell, JB; Gerding, R; Lei, H; Yang, B; Stevens, KL; Hassell, AM; Shewchuk, LM; Leesnitzer, MA; Smith, JL; Sabbatini, P; Atkins, C; Groy, A; Rowand, JL; Kumar, R; Mook, RA; Moorthy, G; Patnaik, S Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg Med Chem Lett 19:360-4 (2009) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM27802
Synonyms:
2-{[2-({1-[2-(diethylamino)acetyl]-5-methoxy-2,3-dihydro-1H-indol-6-yl}amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}-6-fluorobenzamide | pyrrolo[2,3-d]pyrimidine deriv., 26
Type:
Small organic molecule
Emp. Form.:
C28H31FN8O3
Mol. Mass.:
546.5959
SMILES:
CCN(CC)CC(=O)N1CCc2cc(OC)c(Nc3nc(Nc4cccc(F)c4C(N)=O)c4cc[nH]c4n3)cc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotin-GST-c-JUN
Synonyms:
JUN_RAT | Jun | Rjg-9
Type:
Other Protein Type
Mol. Mass.:
8641.27
Organism:
Rattus norvegicus (rat)
Description:
GST-c-Jun (1-79) fusion protein was biotinylated.
Residue:
79
Sequence:
MTAKMETTFYDDALNASFLQSESGAYGYSNPKILKQSMTLNLADPVGNLKPHLRAKNSDLLTSPDVGLLKLASPELERL