Reaction Details Report a problem with these data
Target
Macrophage colony-stimulating factor 1 receptor [538-678,753-922]
Ligand
BDBM4363
Substrate
cFMS -Tie-2 Chimera
Meas. Tech.
cFMs Autophosphorylation Fluorescence Polarization End Point Assay.
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
3300±100 nM
Citation
 Schalk-Hihi, C; Ma, HC; Struble, GT; Bayoumy, S; Williams, R; Devine, E; Petrounia, IP; Mezzasalma, T; Zeng, L; Schubert, C; Grasberger, B; Springer, BA; Deckman, IC Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies. J Biol Chem 282:4085-93 (2007) [PubMed]  Article 
Target
Name:
Macrophage colony-stimulating factor 1 receptor [538-678,753-922]
Synonyms:
6His.FMS.538-922(TIE2) | CSF1R | CSF1R_HUMAN | FMS | Tyrosine Kinase CSF1-R Mutant (Tie2 KID Chimera) | cFMS -Tie-2 Chimera
Type:
Other Protein Type
Mol. Mass.:
37574.75
Organism:
Homo sapiens (Human)
Description:
Recombinant protein contains FMS cytoplasmic domain (FMS538-922.6His), in which FMS KID was replaced with Tie-2 KID.
Residue:
333
Sequence:
GVDYKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKSRVLETDPAFAIANSTASTRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERD
  
Inhibitor
Name:
BDBM4363
Synonyms:
(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enethioamide | AG 213 | CHEMBL77030 | RG-50864 | T7540 (Tyrphostin 47) | Tyrphostin A47 | alpha-Cyano-(3,4-dihydroxy)thiocinnamide | benzylidenemalononitrile (BMN) deriv. 47
Type:
Small organic molecule
Emp. Form.:
C10H8N2O2S
Mol. Mass.:
220.248
SMILES:
NC(=S)C(=C\c1ccc(O)c(O)c1)\C#N
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Macrophage colony-stimulating factor 1 receptor [538-678,753-922]
Synonyms:
6His.FMS.538-922(TIE2) | CSF1R | CSF1R_HUMAN | FMS | Tyrosine Kinase CSF1-R Mutant (Tie2 KID Chimera) | cFMS -Tie-2 Chimera
Type:
Other Protein Type
Mol. Mass.:
37574.75
Organism:
Homo sapiens (Human)
Description:
Recombinant protein contains FMS cytoplasmic domain (FMS538-922.6His), in which FMS KID was replaced with Tie-2 KID.
Residue:
333
Sequence:
GVDYKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKSRVLETDPAFAIANSTASTRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERD