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TargetTyrosine-protein kinase Yes
LigandBDBM50198782
Substrate/Competitorn/a
Meas. Tech.ChEMBL_437758 (CHEMBL905847)
Ki 12.9±n/a nM
Citation Noronha, GBarrett, KBoccia, ABrodhag, TCao, JChow, CPDneprovskaia, EDoukas, JFine, RGong, XGritzen, CGu, HHanna, EHood, JDHu, SKang, XKey, JKlebansky, BKousba, ALi, GLohse, DMak, CCMcPherson, APalanki, MSPathak, VPRenick, JShi, FSoll, RSplittgerber, UStoughton, STang, SYee, SZeng, BZhao, NZhu, H Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. Bioorg Med Chem Lett17:602-8 (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
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BDBM50198782
n/a
NameBDBM50198782
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
TypeSmall organic molecule
Emp. Form.C26H25Cl2N5O
Mol. Mass.494.416
SMILESCc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl
Structure
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