Reaction Details Report a problem with these data
Target
Macrophage colony-stimulating factor 1 receptor [538-972]
Ligand
BDBM2579
Substrate
Macrophage colony-stimulating factor 1 receptor (CSF1R)
Meas. Tech.
cFMs Autophosphorylation Fluorescence Polarization End Point Assay.
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
57±9 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 [538-972]
Synonyms:
CSF1R | CSF1R_HUMAN | FMS | FMS.538-972.6His | Macrophage colony-stimulating factor 1 receptor (aa 538-972)
Type:
n/a
Mol. Mass.:
48843.65
Organism:
n/a
Description:
P07333 aa 538-972
Residue:
435
Sequence:
YKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKAEAMLGPSLSPGQDPEGGVDYKNIHLEKKYVRRDSGFSSQGVDTYVEMRPVSTSSNDSFSEQDLDKEDGRPLELRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERDYTNLPSSSRSGGSGSSSSELEEESSSEHLTCCEQGDIAQPLLQPNNYQFC
 
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
Synonyms:
CSF1R | CSF1R_HUMAN | FMS | Fms proto-oncogene | Macrophage colony stimulating factor receptor | Macrophage colony-stimulating factor 1 receptor (FMS) | Macrophage colony-stimulating factor 1 receptor (c-FMS) | Macrophage colony-stimulating factor 1 receptor (cFMS) | Proto-oncogene c-Fms | Tyrosine Kinase CSF1-R | c-fms | cFMS
Type:
Protein
Mol. Mass.:
107979.48
Organism:
Homo sapiens (Human)
Description:
P07333
Residue:
972
Sequence:
MGPGVLLLLLVATAWHGQGIPVIEPSVPELVVKPGATVTLRCVGNGSVEWDGPPSPHWTLYSDGSSSILSTNNATFQNTGTYRCTEPGDPLGGSAAIHLYVKDPARPWNVLAQEVVVFEDQDALLPCLLTDPVLEAGVSLVRVRGRPLMRHTNYSFSPWHGFTIHRAKFIQSQDYQCSALMGGRKVMSISIRLKVQKVIPGPPALTLVPAELVRIRGEAAQIVCSASSVDVNFDVFLQHNNTKLAIPQQSDFHNNRYQKVLTLNLDQVDFQHAGNYSCVASNVQGKHSTSMFFRVVESAYLNLSSEQNLIQEVTVGEGLNLKVMVEAYPGLQGFNWTYLGPFSDHQPEPKLANATTKDTYRHTFTLSLPRLKPSEAGRYSFLARNPGGWRALTFELTLRYPPEVSVIWTFINGSGTLLCAASGYPQPNVTWLQCSGHTDRCDEAQVLQVWDDPYPEVLSQEPFHKVTVQSLLTVETLEHNQTYECRAHNSVGSGSWAFIPISAGAHTHPPDEFLFTPVVVACMSIMALLLLLLLLLLYKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKAEAMLGPSLSPGQDPEGGVDYKNIHLEKKYVRRDSGFSSQGVDTYVEMRPVSTSSNDSFSEQDLDKEDGRPLELRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERDYTNLPSSSRSGGSGSSSSELEEESSSEHLTCCEQGDIAQPLLQPNNYQFC