Target
Fibroblast growth factor receptor 1
Ligand
BDBM3497
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
68±n/a nM
Citation
 Schroeder, MCHamby, JMConnolly, CJGrohar, PJWinters, RTBarvian, MRMoore, CWBoushelle, SLCrean, SMKraker, AJDriscoll, DLVincent, PWElliott, WLLu, GHBatley, BLDahring, TKMajor, TCPanek, RLDoherty, AMShowalter, HD Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. J Med Chem 44:1915-26 (2001) [PubMed]  Article 
Target
Name:
Fibroblast growth factor receptor 1
Synonyms:
BFGFR | Basic fibroblast growth factor receptor 1 | Basic fibroblast growth factor receptor 1 (FGFR1) | CD_antigen=CD331 | CEK | FGFBR | FGFR-1 | FGFR-1 Tyrosine Kinase | FGFR-1, (FL) | FGFR1 | FGFR1_HUMAN | FLG | FLT2 | Fibroblast growth factor receptor (FGFR) | Fibroblast growth factor receptor 1 (FGFR-1) | Fibroblast growth factor receptor 1 (FGFR1) | Fms-like tyrosine kinase 2 | HBGFR | N-sam | VEGF-receptor 2 and Fibroblast growth factor receptor 1 | bFGF-R | c-fgr
Type:
Receptor
Mol. Mass.:
91861.70
Organism:
Homo sapiens (Human)
Description:
P11362
Residue:
822
Sequence:
MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDDVQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSDALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPSSGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSINHTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKIGPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLEALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKSIPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVLGKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDLVSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNGRLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSFPDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
  
Inhibitor
Name:
BDBM3497
Synonyms:
6-arylpyrido[2,3-d]pyrimidine deriv. 79 | N-[6-(2,6-dichlorophenyl)-2-{[3-(4-methylpiperazin-1-yl)propyl]amino}pyrido[2,3-d]pyrimidin-7-yl]benzenesulfonamide | N-{6-(2,6-Dichloro-phenyl)-2-[3-(4-methylpiperazin-1-yl)-propylamino]-pyrido[2,3-d]pyrimidin-7yl}-benzenesulfonamide
Type:
Small organic molecule
Emp. Form.:
C27H29Cl2N7O2S
Mol. Mass.:
586.536
SMILES:
CN1CCN(CCCNc2ncc3cc(c(NS(=O)(=O)c4ccccc4)nc3n2)-c2c(Cl)cccc2Cl)CC1 |(10.36,-17.58,;11.69,-16.81,;11.69,-15.27,;13.02,-14.5,;14.36,-15.27,;15.69,-14.5,;17.02,-15.27,;18.36,-14.5,;19.69,-15.27,;21.03,-14.5,;21.03,-12.96,;22.36,-12.19,;23.69,-12.96,;25.03,-12.19,;26.36,-12.96,;26.36,-14.5,;27.69,-15.27,;27.69,-16.81,;26.36,-17.58,;29.03,-16.04,;28.46,-18.14,;28.46,-19.68,;29.8,-20.45,;31.13,-19.68,;31.13,-18.14,;29.8,-17.37,;25.03,-15.27,;23.69,-14.5,;22.36,-15.27,;27.69,-12.19,;27.69,-10.65,;26.36,-9.88,;29.03,-9.88,;30.36,-10.65,;30.36,-12.19,;29.03,-12.96,;29.03,-14.5,;14.36,-16.81,;13.02,-17.58,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly(E:Y)
Synonyms:
n/a
Type:
Random polymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
Random copolymer of glutamic acid and tyrosine (4:1). 50 uM ATP containing 0.4 uCi of [gamma-32P]ATP as co-substrate
Residue:
3
Sequence:
NA