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Target
Mast/stem cell growth factor receptor Kit [N822K]
Ligand
BDBM6572
Substrate
BDBM13531
Meas. Tech.
Kinase Assay and Binding Constant Measurement
Kd
4±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:
BDBM6572
Synonyms:
6-(2,6-dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one | PD-180970 | 6-(2,6-dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-7H,8H-pyrido[2,3-d]pyrimidin-7-one | PD180970
Type:
Small organic molecule
Emp. Form.:
C21H15Cl2FN4O
Mol. Mass.:
428.06
SMILES:
Cc1cc(ccc1F)Nc2ncc3c(n2)N(C(=O)C(=C3)c4c(cccc4Cl)Cl)C
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(cc1)-c1nc(c([nH]1)-c1ccc(F)cc1)-c1ccncc1
Structure:
Search PDB for entries with ligand similarity: