Reaction Details Report a problem with these data
Target
Macrophage colony-stimulating factor 1 receptor
Ligand
BDBM27619
Substrate
Biotinylated substrate peptide
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
22±n/a nM
Citation
Burns, CJ; Harte, MF; Bu, X; Fantino, E; Giarrusso, M; Joffe, M; Kurek, M; Legge, FS; Razzino, P; Su, S; Treutlein, H; Wan, SS; Zeng, J; Wilks, AF Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. Bioorg Med Chem Lett 19:1206-9 (2009) [PubMed] Article
More Info.:
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:
BDBM27619
Synonyms:
N-[3-(1-{[6-(4-hydroxy-3-methoxyphenyl)pyrazin-2-yl]amino}ethyl)phenyl]pyridine-3-carboxamide | alpha-methylbenzylamino pyrazine deriv., 1
Type:
Small organic molecule
Emp. Form.:
C25H23N5O3
Mol. Mass.:
441.4818
SMILES:
COc1cc(ccc1O)-c1cncc(NC(C)c2cccc(NC(=O)c3cccnc3)c2)n1
Substrate
Name:
Biotinylated substrate peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2803.42
Organism:
n/a
Description:
n/a
Residue:
23
Sequence:
ITINEGPWLEEEEEAYGWMDFNH