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Target
Mitogen-activated protein kinase 10
Ligand
BDBM50314070
Substrate
n/a
Meas. Tech.
ChEMBL_742477 (CHEMBL1769125)
Kd
19±n/a nM
Citation
 Goldstein, DM; Soth, M; Gabriel, T; Dewdney, N; Kuglstatter, A; Arzeno, H; Chen, J; Bingenheimer, W; Dalrymple, SA; Dunn, J; Farrell, R; Frauchiger, S; La Fargue, J; Ghate, M; Graves, B; Hill, RJ; Li, F; Litman, R; Loe, B; McIntosh, J; McWeeney, D; Papp, E; Park, J; Reese, HF; Roberts, RT; Rotstein, D; San Pablo, B; Sarma, K; Stahl, M; Sung, ML; Suttman, RT; Sjogren, EB; Tan, Y; Trejo, A; Welch, M; Weller, P; Wong, BR; Zecic, H Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors J Med Chem 54:2255-65 (2011) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 10
Synonyms:
JNK3 | JNK3A | MAP kinase p49 3F12 | MAPK10 | MK10_HUMAN | Mitogen-Activated Protein Kinase 10 (JNK3) | Mitogen-activated protein kinase 10 (Stress-activated protein kinase JNK3) (c-Jun N-terminal kinase 3) (MAP kinase p49 3F12) | Mitogen-activated protein kinase 10/Receptor-interacting serine/threonine-protein kinase 1 | PRKM10 | SAPK1B | Stress-activated protein kinase JNK3 | c-Jun N-terminal kinase 3 (JNK3)
Type:
Enzyme
Mol. Mass.:
52586.89
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
464
Sequence:
MSLHFLYYCSEPTLDVKIAFCQGFDKQVDVSYIAKHYNMSKSKVDNQFYSVEVGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAVLDRNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIISLLNVFTPQKTLEEFQDVYLVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDIWSVGCIMGEMVRHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRNYVENRPKYAGLTFPKLFPDSLFPADSEHNKLKASQARDLLSKMLVIDPAKRISVDDALQHPYINVWYDPAEVEAPPPQIYDKQLDEREHTIEEWKELIYKEVMNSEEKTKNGVVKGQPSPSGAAVNSSESLPPSSSVNDISSMSTDQTLASDTDSSLEASAGPLGCCR
  
Inhibitor
Name:
BDBM50314070
Synonyms:
6-(2,4-difluorophenoxy)-2-{[3-hydroxy-1-(2-hydroxyethyl)propyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1090089 | pamapimod
Type:
Small organic molecule
Emp. Form.:
C19H20F2N4O4
Mol. Mass.:
406.3833
SMILES:
Cn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure:
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