Reaction Details Report a problem with these data
Target
Macrophage colony-stimulating factor 1 receptor
Ligand
BDBM27912
Substrate
FMS Substrate Peptide
Meas. Tech.
FMS Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
0.3±n/a nM
Citation
 Huang, H; Hutta, DA; Rinker, JM; Hu, H; Parsons, WH; Schubert, C; Desjarlais, RL; Crysler, CS; Chaikin, MA; Donatelli, RR; Chen, Y; Cheng, D; Zhou, Z; Yurkow, E; Manthey, CL; Player, MR Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). J Med Chem 52:1081-99 (2009) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM27912
Synonyms:
8-(4-ethylphenyl)-N-methoxy-2-{[4-(1-methylpiperidin-4-yl)phenyl]amino}-5-oxo-5H,8H-pyrido[2,3-d]pyrimidine-6-carboxamide | Pyrido[2,3-d]pyrimidin-5-one, 45
Type:
Small organic molecule
Emp. Form.:
C29H32N6O3
Mol. Mass.:
512.6028
SMILES:
CCc1ccc(cc1)-n1cc(C(=O)NOC)c(=O)c2cnc(Nc3ccc(cc3)C3CCN(C)CC3)nc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Macrophage colony-stimulating factor 1 receptor [555-568]
Synonyms:
CSF1R | CSF1R_HUMAN | FMS | FMS (aa 555-568) peptide | FMS Substrate Peptide (aa 555-568) | Macrophage colony-stimulating factor 1 receptor (CSF1R) or (c-fms)
Type:
Peptide
Mol. Mass.:
1619.64
Organism:
Homo sapiens (Human)
Description:
P07333 aa 555-568
Residue:
14
Sequence:
SYEGNSYTFIDPTQ