| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Serine/threonine-protein kinase B-raf |
|---|
| Ligand | BDBM50428286 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1495744 (CHEMBL3578907) |
|---|
| IC50 | 6.0±n/a nM |
|---|
| Citation |  Henry, JR; Kaufman, MD; Peng, SB; Ahn, YM; Caldwell, TM; Vogeti, L; Telikepalli, H; Lu, WP; Hood, MM; Rutkoski, TJ; Smith, BD; Vogeti, S; Miller, D; Wise, SC; Chun, L; Zhang, X; Zhang, Y; Kays, L; Hipskind, PA; Wrobleski, AD; Lobb, KL; Clay, JM; Cohen, JD; Walgren, JL; McCann, D; Patel, P; Clawson, DK; Guo, S; Manglicmot, D; Groshong, C; Logan, C; Starling, JJ; Flynn, DL Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J Med Chem58:4165-79 (2015) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Serine/threonine-protein kinase B-raf |
|---|
| Name: | Serine/threonine-protein kinase B-raf |
|---|
| Synonyms: | B-RAF | B-Raf Protein Kinase | B-Raf proto-oncogene serine/threonine-protein kinase | BRAF | BRAF1 | BRAF_HUMAN | RAFB1 | p94 | v-Raf murine sarcoma viral oncogene homolog B1 |
|---|
| Type: | Serine/threonine-protein kinase |
|---|
| Mol. Mass.: | 84446.00 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P15056 |
|---|
| Residue: | 766 |
|---|
| Sequence: | MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
|
|
|
|---|
| BDBM50428286 |
|---|
| n/a |
|---|
| Name | BDBM50428286 |
|---|
| Synonyms: | DABRAFENIB | GSK2118436A |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C23H20F3N5O2S2 |
|---|
| Mol. Mass. | 519.562 |
|---|
| SMILES | CC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F |
|---|
| Structure | 
|
|---|
Search and Browse
