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Target
Macrophage colony-stimulating factor 1 receptor
Ligand
BDBM27895
Substrate
FMS Substrate Peptide
Meas. Tech.
FMS Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
0.7±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:
Human
Description:
P07333
Residue:
972
Sequence:
MGPGVLLLLLVATAWHGQGIPVIEPSVPELVVKPGATVTLRCVGNGSVEWDGPPSPHWTLYSDGSSSILSTNNATFQNTGTYRCTEPGDPLGGSAAIHLYVKDPARPWNVLAQEVVVFEDQDALLPCLLTDPVLEAGVSLVRVRGRPLMRHTNYSFSPWHGFTIHRAKFIQSQDYQCSALMGGRKVMSISIRLKVQKVIPGPPALTLVPAELVRIRGEAAQIVCSASSVDVNFDVFLQHNNTKLAIPQQSDFHNNRYQKVLTLNLDQVDFQHAGNYSCVASNVQGKHSTSMFFRVVESAYLNLSSEQNLIQEVTVGEGLNLKVMVEAYPGLQGFNWTYLGPFSDHQPEPKLANATTKDTYRHTFTLSLPRLKPSEAGRYSFLARNPGGWRALTFELTLRYPPEVSVIWTFINGSGTLLCAASGYPQPNVTWLQCSGHTDRCDEAQVLQVWDDPYPEVLSQEPFHKVTVQSLLTVETLEHNQTYECRAHNSVGSGSWAFIPISAGAHTHPPDEFLFTPVVVACMSIMALLLLLLLLLLYKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKAEAMLGPSLSPGQDPEGGVDYKNIHLEKKYVRRDSGFSSQGVDTYVEMRPVSTSSNDSFSEQDLDKEDGRPLELRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERDYTNLPSSSRSGGSGSSSSELEEESSSEHLTCCEQGDIAQPLLQPNNYQFC
Inhibitor
Name:
BDBM27895
Synonyms:
8-(2,3-dihydro-1H-inden-5-yl)-N-methoxy-2-({4-[2-(4-methylpiperazin-1-yl)ethyl]phenyl}amino)-5-oxo-5H,8H-pyrido[2,3-d]pyrimidine-6-carboxamide | Pyrido[2,3-d]pyrimidin-5-one, 18a
Type:
Small organic molecule
Emp. Form.:
C31H35N7O3
Mol. Mass.:
553.6547
SMILES:
CONC(=O)c1cn(-c2ccc3CCCc3c2)c2nc(Nc3ccc(CCN4CCN(C)CC4)cc3)ncc2c1=O
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:
Human
Description:
P07333 aa 555-568
Residue:
14
Sequence:
SYEGNSYTFIDPTQ