Reaction Details Report a problem with these data
Target
Macrophage colony-stimulating factor 1 receptor [538-678,753-922]
Ligand
BDBM2579
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
49±4 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:
BDBM2579
Synonyms:
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.531
SMILES:
CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
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