Target
Mast/stem cell growth factor receptor Kit
Ligand
BDBM50253152
Substrate
n/a
Meas. Tech.
ChEMBL_539860 (CHEMBL1024856)
IC50
1174±n/a nM
Citation
 Herberich, BCao, GQChakrabarti, PPFalsey, JRPettus, LRzasa, RMReed, ABReichelt, ASham, KThaman, MWurz, RPXu, SZhang, DHsieh, FLee, MRSyed, RLi, VGrosfeld, DPlant, MHHenkle, BSherman, LMiddleton, SWong, LMTasker, AS Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold. J Med Chem 51:6271-9 (2008) [PubMed]  Article 
Target
Name:
Mast/stem cell growth factor receptor Kit
Synonyms:
CD117 antigen | CD_antigen=CD117 | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (cKIT) | Proto-oncogene c-Kit | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Stem cell growth factor receptor | Tyrosine Kinase c-Kit | Tyrosine-protein kinase Kit | Tyrosine-protein kinase Kit (c-Kit) | c-kit | p-145 c-kit | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Type:
Protein
Mol. Mass.:
109869.37
Organism:
Homo sapiens (Human)
Description:
P10721
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM50253152
Synonyms:
CHEMBL493708 | N-Cyclopropyl-4-methyl-3-(1-((R)-2,2,2-trifluoro-1-methylethoxy)-6-phthalazinyl)benzamide
Type:
Small organic molecule
Emp. Form.:
C22H20F3N3O2
Mol. Mass.:
415.4083
SMILES:
C[C@@H](Oc1nncc2cc(ccc12)-c1cc(ccc1C)C(=O)NC1CC1)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: