Reaction Details
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RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM50339625
Substrate
n/a
Meas. Tech.
ChEMBL_734962 (CHEMBL1693569)
IC50
16±n/a nM
Citation
Gould, AE; Adams, R; Adhikari, S; Aertgeerts, K; Afroze, R; Blackburn, C; Calderwood, EF; Chau, R; Chouitar, J; Duffey, MO; England, DB; Farrer, C; Forsyth, N; Garcia, K; Gaulin, J; Greenspan, PD; Guo, R; Harrison, SJ; Huang, SC; Iartchouk, N; Janowick, D; Kim, MS; Kulkarni, B; Langston, SP; Liu, JX; Ma, LT; Menon, S; Mizutani, H; Paske, E; Renou, CC; Rezaei, M; Rowland, RS; Sintchak, MD; Smith, MD; Stroud, SG; Tregay, M; Tian, Y; Veiby, OP; Vos, TJ; Vyskocil, S; Williams, J; Xu, T; Yang, JJ; Yano, J; Zeng, H; Zhang, DM; Zhang, Q; Galvin, KM Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem 54:1836-46 (2011) [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:
BDBM50339625
Synonyms:
4-{[7-({[4-(Aminomethyl)-3-(trifluoromethyl)phenyl]amino}carbonyl)-5,6,7,8-tetrahydronaphthalen-2-yl]oxy}-Nmethylpyridine-2-carboxamide | CHEMBL1688865
Type:
Small organic molecule
Emp. Form.:
C26H25F3N4O3
Mol. Mass.:
498.4969
SMILES:
CNC(=O)c1cc(Oc2ccc3CCC(Cc3c2)C(=O)Nc2ccc(CN)c(c2)C(F)(F)F)ccn1
Structure:
