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Target
Mitogen-activated protein kinase 8
Ligand
BDBM50334002
Substrate
n/a
Meas. Tech.
ChEMBL_701207 (CHEMBL1648827)
IC50
4200±n/a nM
Citation
 Probst, GD; Bowers, S; Sealy, JM; Truong, AP; Hom, RK; Galemmo, RA; Konradi, AW; Sham, HL; Quincy, DA; Pan, H; Yao, N; Lin, M; Tóth, G; Artis, DR; Zmolek, W; Wong, K; Qin, A; Lorentzen, C; Nakamura, DF; Quinn, KP; Sauer, JM; Powell, K; Ruslim, L; Wright, S; Chereau, D; Ren, Z; Anderson, JP; Bard, F; Yednock, TA; Griswold-Prenner, I Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration. Bioorg Med Chem Lett 21:315-9 (2010) [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:
BDBM50334002
Synonyms:
4-(6-bromonaphthalen-2-yl)-3-(2-(tetrahydro-2H-pyran-4-ylamino)pyridin-4-yl)-1H-1,2,4-triazol-5(4H)-one | CHEMBL1644634
Type:
Small organic molecule
Emp. Form.:
C22H20BrN5O2
Mol. Mass.:
466.331
SMILES:
Brc1ccc2cc(ccc2c1)-n1c(n[nH]c1=O)-c1ccnc(NC2CCOCC2)c1
Structure:
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