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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50314051
Substrate
n/a
Meas. Tech.
ChEMBL_627145 (CHEMBL1111787)
IC50
>50000±n/a nM
Citation
 Gopalsamy, A; Ciszewski, G; Shi, M; Berger, D; Hu, Y; Lee, F; Feldberg, L; Frommer, E; Kim, S; Collins, K; Wojciechowicz, D; Mallon, R Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. Bioorg Med Chem Lett 19:6890-2 (2009) [PubMed]  Article
Target
Name:
Mitogen-activated protein kinase kinase kinase 8
Synonyms:
C-COT | COT | COT proto-oncogene serine/threonine-protein kinase | Cancer Osaka thyroid oncogene | ESTF | M3K8_HUMAN | MAP3K8 | Tpl-2 | Tumor Progression Loci-2 Kinase (COT) | Tumor progression locus 2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
52916.89
Organism:
Homo sapiens (Human)
Description:
P41279
Residue:
467
Sequence:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERSKSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGRYQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVEIQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKGLDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVILCRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPGMRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELPENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
  
Inhibitor
Name:
BDBM50314051
Synonyms:
CHEMBL1089082 | N-(3-(2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamide
Type:
Small organic molecule
Emp. Form.:
C25H16F3N5O
Mol. Mass.:
459.4226
SMILES:
FC(F)(F)c1cccc(c1)C(=O)Nc1cccc(c1)-c1ccnc2cc(nn12)-c1ccncc1
Structure:
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