Target
Mast/stem cell growth factor receptor Kit [V559D,T670I]
Ligand
BDBM13530
Substrate
BDBM13531
Meas. Tech.
Kinase Assay and Binding Constant Measurement
Kd
3000±n/a nM
Citation
 Carter, TAWodicka, LMShah, NPVelasco, AMFabian, MATreiber, DKMilanov, ZVAtteridge, CEBiggs, WHEdeen, PTFloyd, MFord, JMGrotzfeld, RMHerrgard, SInsko, DEMehta, SAPatel, HKPao, WSawyers, CLVarmus, HZarrinkar, PPLockhart, 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:
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:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKDVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVIIEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM13530
Synonyms:
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide | CHEMBL941 | Gleevec | Imatinib | Imatinib, 21 | N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]benzamide | STI-571 | STI571 | US10906896, Cpd imatinib | US11649218, Example Imatinib | US11725005, Compound imatinib | US9255107, Imatinib | cid_5291 | imatinib-CD3 | med.21724, Compound 6
Type:
Small organic molecule
Emp. Form.:
C29H31N7O
Mol. Mass.:
493.6027
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-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole | 4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol | 4-[4-(4-fluorophenyl)-5-(4-pyridyl)-4-imidazolin-2-ylidene]cyclohexa-2,5-dien-1-one | 4-[5-(4-fluorophenyl)-4-(pyridin-4-yl)-1H-imidazol-2-yl]phenol | SB-202190 | SB202190 | biotinylated SB202190
Type:
Small organic molecule
Emp. Form.:
C20H14FN3O
Mol. Mass.:
331.3431
SMILES:
Oc1ccc(cc1)-c1nc(c([nH]1)-c1ccc(F)cc1)-c1ccncc1
Structure:
Search PDB for entries with ligand similarity: