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Target
RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM50307880
Substrate
n/a
Meas. Tech.
ChEMBL_612864 (CHEMBL1067553)
IC50
126±n/a nM
Citation
Nourry, A; Zambon, A; Davies, L; Niculescu-Duvaz, I; Dijkstra, HP; Ménard, D; Gaulon, C; Niculescu-Duvaz, D; Suijkerbuijk, BM; Friedlos, F; Manne, HA; Kirk, R; Whittaker, S; Marais, R; Springer, CJ BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. J Med Chem 53:1964-78 (2010) [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:
Homo sapiens (Human)
Description:
P04049
Residue:
648
Sequence:
MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRVFLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAASLIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKVPTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTFNTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNLSPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSFGTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIVTQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGLTVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYELMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFPQILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
Inhibitor
Name:
BDBM50307880
Synonyms:
CHEMBL598626 | N-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yloxy)benzamide
Type:
Small organic molecule
Emp. Form.:
C27H25N5O3
Mol. Mass.:
467.5191
SMILES:
CC(C)(C)c1cc(NC(=O)c2cccc(Oc3cccc4[nH]c(=O)[nH]c34)c2)n(n1)-c1ccccc1