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Target
RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM26036
Substrate
MEK Inactive Mutant
Meas. Tech.
RAF Kinase Inhibition Assay
IC50
17±n/a nM
Citation
Ramurthy, S; Subramanian, S; Aikawa, M; Amiri, P; Costales, A; Dove, J; Fong, S; Jansen, JM; Levine, B; Ma, S; McBride, CM; Michaelian, J; Pick, T; Poon, DJ; Girish, S; Shafer, CM; Stuart, D; Sung, L; Renhowe, PA Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors. J Med Chem 51:7049-52 (2008) [PubMed] Article
More Info.:
Target
Name:
RAF proto-oncogene serine/threonine-protein kinase
Synonyms:
C-Raf Protein Kinase | Proto-oncogene c-RAF (RAF1) | RAF | RAF proto-oncogene
serine/threonine-protein kinase (C-Raf) | RAF1 | RAF1_HUMAN | Raf-1 | Serine/threonine-protein kinase
RAF | Serine/threonine-protein kinase C-Raf | cRaf
Type:
Serine/threonine-protein kinase
Mol. Mass.:
73082.52
Organism:
Human
Description:
P04049
Residue:
648
Sequence:
MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRVFLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAASLIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKVPTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTFNTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNLSPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSFGTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIVTQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGLTVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYELMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFPQILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
Inhibitor
Name:
BDBM26036
Synonyms:
4-({2-[(4-bromophenyl)amino]-1-methyl-1H-1,3-benzodiazol-5-yl}oxy)-N-[2-(morpholin-4-yl)ethyl]pyridine-2-carboxamide | arylaminobenzimidazole, 31
Type:
Small organic molecule
Emp. Form.:
C26H27BrN6O3
Mol. Mass.:
551.435
SMILES:
Cn1c(Nc2ccc(Br)cc2)nc2cc(Oc3ccnc(c3)C(=O)NCCN3CCOCC3)ccc12
Substrate
Name:
MEK Inactive Mutant
Synonyms:
Full length kinase dead MEK | kd-MEK
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA