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Target
Mast/stem cell growth factor receptor Kit [V559D,T670I]
Ligand
BDBM13533
Substrate
BDBM13531
Meas. Tech.
Kinase Assay and Binding Constant Measurement
Kd
300±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 [V559D,T670I]
Synonyms:
Proto-oncogene tyrosine-protein kinase Kit | CD117 antigen | Mast/stem cell growth factor receptor precursor | Tyrosine Kinase c-Kit Mutant (V559D/T670I) | KIT_HUMAN | KIT | SCFR | Mast/stem cell growth factor receptor Kit (V559D/T670I)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
109896.38
Organism:
Human
Description:
P10721[V559D,T670I]
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKDVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVIIEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM13533
Synonyms:
1-[5-tert-butyl-2-(p-tolyl)pyrazol-3-yl]-3-[4-(2-morpholinoethoxy)-1-naphthyl]urea | US8933228, BIRB 796 | cid_156422 | BIRB-796, 3 | 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | BIRB 796 | diaryl urea compound 10 | 3-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-1-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 1-[5-tert-butyl-2-(4-methylphenyl)-3-pyrazolyl]-3-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea | CHEMBL103667 | 1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 3-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]-1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}urea | Doramapimod | BIRB-796 | US9187470, 43 (BIRB-796) | US9242960, BIRB 796 | US9260410, BIRB796 | US11407771, Compound 43 | D3RKN_73
Type:
Small organic molecule
Emp. Form.:
C31H37N5O3
Mol. Mass.:
527.29
SMILES:
Cc1ccc(cc1)-n1nc(cc1NC(=O)Nc1ccc(OCCN2CCOCC2)c2ccccc12)C(C)(C)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(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1
Structure:
Search PDB for entries with ligand similarity: