Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 14
Ligand
BDBM16343
Substrate
biotinylated GST-ATF2
Meas. Tech.
Enzyme Inhibition Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
14.6±n/a nM
Citation
McClure, KF; Letavic, MA; Kalgutkar, AS; Gabel, CA; Audoly, L; Barberia, JT; Braganza, JF; Carter, D; Carty, TJ; Cortina, SR; Dombroski, MA; Donahue, KM; Elliott, NC; Gibbons, CP; Jordan, CK; Kuperman, AV; Labasi, JM; Laliberte, RE; McCoy, JM; Naiman, BM; Nelson, KL; Nguyen, HT; Peese, KM; Sweeney, FJ; Taylor, TJ; Trebino, CE; Abramov, YA; Laird, ER; Volberg, WA; Zhou, J; Bach, J; Lombardo, F Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development. Bioorg Med Chem Lett 16:4339-44 (2006) [PubMed] Article
More Info.:
Target
Name:
Mitogen-activated protein kinase 14
Synonyms:
CSAID-binding protein | CSBP | CSBP1 | CSBP2 | CSPB1 | Cytokine suppressive anti-inflammatory drug-binding protein | MAP kinase 14 | MAP kinase MXI2 | MAP kinase p38 alpha | MAPK 14 | MAPK14 | MAX-interacting protein 2 | MK14_HUMAN | MXI2 | Mitogen-activated protein kinase p38 alpha | SAPK2A | Stress-activated protein kinase 2a | p38 MAP kinase alpha/beta
Type:
Serine/threonine-protein kinase
Mol. Mass.:
41286.76
Organism:
Homo sapiens (Human)
Description:
Q16539
Residue:
360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
Inhibitor
Name:
BDBM16343
Synonyms:
4-(2,6-difluorophenyl)-5-[3-(propan-2-yl)-[1,2,4]triazolo[3,4-a]pyridin-6-yl]-1,3-oxazole | triazolopyridine oxazole inhibitor 13
Type:
Small organic molecule
Emp. Form.:
C18H14F2N4O
Mol. Mass.:
340.3268
SMILES:
CC(C)c1nnc2ccc(cn12)-c1ocnc1-c1c(F)cccc1F |(-5.34,-5.49,;-4.57,-4.15,;-3.03,-4.15,;-5.34,-2.82,;-6.87,-2.98,;-7.5,-1.57,;-6.35,-.54,;-6.35,1,;-5.02,1.77,;-3.69,1,;-3.69,-.54,;-5.02,-1.31,;-2.52,2,;-1.02,1.64,;-.22,2.96,;-1.22,4.13,;-2.64,3.53,;-3.97,4.3,;-3.97,5.85,;-2.64,6.62,;-5.31,6.62,;-6.64,5.85,;-6.64,4.3,;-5.31,3.53,;-5.31,1.99,)|
Substrate
Name:
biotinylated GST-ATF2
Synonyms:
ATF-2-GST | ATF2 | Activating transcription factor 2 | Activating transcription factor 2-GST fusion | GST-ATF2 | biotinylated ATF2 substrate | biotinylated activating transcription factor 2
Type:
Other Protein Type
Mol. Mass.:
12237.77
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
109
Sequence:
MSDDKPFLCTAPGCGQRFTNEDHLAVHKHKHEMTLKFGPARNDSVIVADQTPTPTRFLKNCEEVGLFNELASPFENEFKKASEDDIKKMPLDLSPLATPIIRSKIEEPS