| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret |
|---|
| Ligand | BDBM50198782 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_437766 (CHEMBL905855) |
|---|
| Ki | 407±n/a nM |
|---|
| Citation |  Noronha, G; Barrett, K; Boccia, A; Brodhag, T; Cao, J; Chow, CP; Dneprovskaia, E; Doukas, J; Fine, R; Gong, X; Gritzen, C; Gu, H; Hanna, E; Hood, JD; Hu, S; Kang, X; Key, J; Klebansky, B; Kousba, A; Li, G; Lohse, D; Mak, CC; McPherson, A; Palanki, MS; Pathak, VP; Renick, J; Shi, F; Soll, R; Splittgerber, U; Stoughton, S; Tang, S; Yee, S; Zeng, B; Zhao, N; Zhu, 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 |
|---|
| |
| Proto-oncogene tyrosine-protein kinase receptor Ret |
|---|
| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret |
|---|
| Synonyms: | CDHF12 | CDHR16 | Cadherin family member 12 | PTC | Proto-oncogene c-Ret | RET | RET51 | RET_HUMAN | Tyrosine-protein kinase Ret (RET) |
|---|
| Type: | Protein |
|---|
| Mol. Mass.: | 124318.29 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P07949 |
|---|
| Residue: | 1114 |
|---|
| Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
|
|
|
|---|
| 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 | 
|
|---|
Search and Browse
