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Target
Mast/stem cell growth factor receptor Kit [N822K]
Ligand
BDBM13530
Substrate
BDBM13531
Meas. Tech.
Kinase Assay and Binding Constant Measurement
Kd
3±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 A 102:11011-6 (2005) [PubMed]  Article 
Target
Name:
Mast/stem cell growth factor receptor Kit [N822K]
Synonyms:
KIT_HUMAN | KIT | SCFR | CD117 antigen | Mast/stem cell growth factor receptor precursor | Proto-oncogene tyrosine-protein kinase Kit | Tyrosine Kinase c-Kit Mutant (N822K)
Type:
Enzyme
Mol. Mass.:
109884.45
Organism:
Human
Description:
P10721[N822K]
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSKYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM13530
Synonyms:
cid_5291 | STI571 | N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]benzamide | Gleevec | Imatinib, 21 | CHEMBL941 | 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide | STI-571 | Imatinib | US9255107, Imatinib | med.21724, Compound 6 | US10906896, Cpd imatinib | US11649218, Example Imatinib | US11725005, Compound imatinib | US20250129067, Compound Imatinib
Type:
Small organic molecule
Emp. Form.:
C29H31N7O
Mol. Mass.:
493.26
SMILES:
CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM13531
Synonyms:
4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol | SB-202190 | SB202190 | 4-[5-(4-fluorophenyl)-4-(pyridin-4-yl)-1H-imidazol-2-yl]phenol | 4-[4-(4-fluorophenyl)-5-(4-pyridyl)-4-imidazolin-2-ylidene]cyclohexa-2,5-dien-1-one | 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole | biotinylated SB202190
Type:
Small organic molecule
Emp. Form.:
C20H14FN3O
Mol. Mass.:
331.11
SMILES:
Oc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1
Structure:
Search PDB for entries with ligand similarity: