Reaction Details |
| Report a problem with these data |
Target | Tyrosine-protein kinase Yes |
---|
Ligand | BDBM50198782 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_478599 (CHEMBL922440) |
---|
Ki | 12.9±n/a nM |
---|
Citation | Hu, SX; Soll, R; Yee, S; Lohse, DL; Kousba, A; Zeng, B; Yu, X; McPherson, A; Renick, J; Cao, J; Tabak, A; Hood, J; Doukas, J; Noronha, G; Martin, M Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr Drug Metab Dispos35:929-36 (2007) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Tyrosine-protein kinase Yes |
---|
Name: | Tyrosine-protein kinase Yes |
Synonyms: | Proto-oncogene c-Yes | VHL/Tyrosine-protein kinase Yes | YES | YES1 | YES_HUMAN | p61-yes |
Type: | Protein |
Mol. Mass.: | 60801.54 |
Organism: | Homo sapiens (Human) |
Description: | P07947 |
Residue: | 543 |
Sequence: | MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMT
PFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQI
INNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRG
IFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHY
TEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTT
KVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFL
KEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARL
IEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNRE
VLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPG
ENL
|
|
|
BDBM50198782 |
---|
n/a |
---|
Name | BDBM50198782 |
Synonyms: | ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) | 7-(2,6-dichlorophenyl)-5-methyl-N-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)benzo[e][1,2,4]triazin-3-amine | 7-(2,6-dichlorophenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)-phenyl]-1,2,4-benzotriazin-3-amine | CHEMBL230686 | TG-100435 | US8481536, 367 | US8481536, 575 |
Type | Small organic molecule |
Emp. Form. | C26H25Cl2N5O |
Mol. Mass. | 494.416 |
SMILES | Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl |
Structure |
|