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Target
RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM202780
Substrate
n/a
Meas. Tech.
ChEMBL_1663046 (CHEMBL4012727)
EC50
250±n/a nM
Citation
 Nishiguchi, GA; Rico, A; Tanner, H; Aversa, RJ; Taft, BR; Subramanian, S; Setti, L; Burger, MT; Wan, L; Tamez, V; Smith, A; Lou, Y; Barsanti, PA; Appleton, BA; Mamo, M; Tandeske, L; Dix, I; Tellew, JE; Huang, S; Mathews Griner, LA; Cooke, VG; Van Abbema, A; Merritt, H; Ma, S; Gampa, K; Feng, F; Yuan, J; Wang, Y; Haling, JR; Vaziri, S; Hekmat-Nejad, M; Jansen, JM; Polyakov, V; Zang, R; Sethuraman, V; Amiri, P; Singh, M; Lees, E; Shao, W; Stuart, DD; Dillon, MP; Ramurthy, S Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem 60:4869-4881 (2017) [PubMed]  Article 
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:
BDBM202780
Synonyms:
US10245267, Example 127 | US10709712, Example 127 | US9242969, 127 | US9694016, 127
Type:
Small organic molecule
Emp. Form.:
C24H23F3N4O3
Mol. Mass.:
472.4596
SMILES:
COc1ncc(cc1N1CCOCC1)-c1cc(NC(=O)c2cccc(c2)C(F)(F)F)cnc1C
Structure:
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