| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Mast/stem cell growth factor receptor Kit [V559D,T670I] |
|---|
| Ligand | BDBM13534 |
|---|
| Substrate/Competitor | BDBM13531 |
|---|
| Meas. Tech. | Kinase Assay and Binding Constant Measurement |
|---|
| Kd | 600±n/a nM |
|---|
| Citation |  Carter, TA; Wodicka, LM; Shah, NP; Velasco, AM; Fabian, MA; Treiber, DK; Milanov, ZV; Atteridge, CE; Biggs, WH; Edeen, PT; Floyd, M; Ford, JM; Grotzfeld, RM; Herrgard, S; Insko, DE; Mehta, SA; Patel, HK; Pao, W; Sawyers, CL; Varmus, H; Zarrinkar, PP; Lockhart, DJ Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A102:11011-6 (2005) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Mast/stem cell growth factor receptor Kit [V559D,T670I] |
|---|
| Name: | Mast/stem cell growth factor receptor Kit [V559D,T670I] |
|---|
| Synonyms: | CD117 antigen | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (V559D/T670I) | Mast/stem cell growth factor receptor precursor | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Tyrosine Kinase c-Kit Mutant (V559D/T670I) |
|---|
| Type: | Enzyme Catalytic Domain |
|---|
| Mol. Mass.: | 109896.38 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P10721[V559D,T670I] |
|---|
| Residue: | 976 |
|---|
| Sequence: | MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKDVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVIIEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV
|
|
|
|---|
| BDBM13534 |
|---|
| BDBM13531 |
|---|
| Name | BDBM13534 |
|---|
| Synonyms: | CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]thio]phenyl]cyclopropanecarboxamide | VX-680 | VX680 | cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2ylsulphanyl]-phenyl}-amide |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C23H28N8OS |
|---|
| Mol. Mass. | 464.586 |
|---|
| SMILES | CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1 |
|---|
| Structure | 
|
|---|
Search and Browse
