Reaction Details
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RAF proto-oncogene serine/threonine-protein kinase
Ligand
BDBM202839
Substrate
n/a
Meas. Tech.
ChEMBL_1842492 (CHEMBL4342919)
IC50
1.1±n/a nM
Citation
Ramurthy, S; Taft, BR; Aversa, RJ; Barsanti, PA; Burger, MT; Lou, Y; Nishiguchi, GA; Rico, A; Setti, L; Smith, A; Subramanian, S; Tamez, V; Tanner, H; Wan, L; Hu, C; Appleton, BA; Mamo, M; Tandeske, L; Tellew, JE; Huang, S; Yue, Q; Chaudhary, A; Tian, H; Iyer, R; Hassan, AQ; Mathews Griner, LA; La Bonte, LR; Cooke, VG; Van Abbema, A; Merritt, H; Gampa, K; Feng, F; Yuan, J; Mishina, Y; Wang, Y; Haling, JR; Vaziri, S; Hekmat-Nejad, M; Polyakov, V; Zang, R; Sethuraman, V; Amiri, P; Singh, M; Sellers, WR; Lees, E; Shao, W; Dillon, MP; Stuart, DD Design and Discovery of J Med Chem 63:2013-2027 (2020) [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:
BDBM202839
Synonyms:
US10245267, Example 640 | US10709712, Example 191 | US9242969, 191 | US9694016, 640
Type:
Small organic molecule
Emp. Form.:
C26H28N6O3
Mol. Mass.:
472.5389
SMILES:
Cc1ccc(NC(=O)c2ccnc(c2)C(C)(C)C#N)cc1-c1cc(N2CCOCC2)c(=O)n(C)n1
Structure:
