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Target
Macrophage colony-stimulating factor 1 receptor
Ligand
BDBM50589666
Substrate
n/a
Meas. Tech.
ChEMBL_2194014 (CHEMBL5106374)
IC50
12±n/a nM
Citation
 Caldwell, TM; Ahn, YM; Bulfer, SL; Leary, CB; Hood, MM; Lu, WP; Vogeti, L; Vogeti, S; Kaufman, MD; Wise, SC; Le Bourdonnec, B; Smith, BD; Flynn, DL Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT). Bioorg Med Chem Lett 74:0 (2022) [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:
BDBM50589666
Synonyms:
CHEMBL5189742
Type:
Small organic molecule
Emp. Form.:
C23H25N7O2
Mol. Mass.:
431.4903
SMILES:
CCn1cc(cn1)-c1cc(Oc2ccc(nc2C)-c2cnc(NC(C)C)[nH]c2=O)ccn1
Structure:
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