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Target
RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM483981
Substrate
n/a
Meas. Tech.
Kinase Assay
IC50
<0.1±n/a nM
Citation
 Kaldor, SW; Kanouni, T; Arnold, L Inhibitors of RAF kinases US Patent  US10927111 Publication Date 2/23/2021 
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:
BDBM483981
Synonyms:
(R)—N-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and (S)—N-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide | US10927111, Example 17 | US10927111, Example 18 | US10927111, Example 19 | US10927111, Example 20 | US10927111, Example 30 | US10927111, Example 31 | US11667634, Example 20
Type:
Small organic molecule
Emp. Form.:
C23H24F4N6O
Mol. Mass.:
476.4699
SMILES:
CNc1ncc2cc(c(C)nc2n1)-c1cc(NC(=O)N2CC[C@H](CC(F)(F)F)C2)c(F)cc1C |r|
Structure:
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