Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM3066
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
240±n/a nM
Citation
 Klutchko, SR; Hamby, JM; Boschelli, DH; Wu, Z; Kraker, AJ; Amar, AM; Hartl, BG; Shen, C; Klohs, WD; Steinkampf, RW; Driscoll, DL; Nelson, JM; Elliott, WL; Roberts, BJ; Stoner, CL; Vincent, PW; Dykes, DJ; Panek, RL; Lu, GH; Major, TC; Dahring, TK; Hallak, H; Bradford, LA; Showalter, HD; Doherty, AM 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity. J Med Chem 41:3276-92 (1998) [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:
BDBM3066
Synonyms:
2-aminopyrido[2,3-d]pyrimidin-7(8H)-one 33 | 6-(2,6-dichlorophenyl)-8-methyl-2-{[5-(4-methylpiperazin-1-yl)pentyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | PD 166285 analog
Type:
Small organic molecule
Emp. Form.:
C24H30Cl2N6O
Mol. Mass.:
489.441
SMILES:
CN1CCN(CCCCCNc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)CC1 |(-9.18,-13.72,;-9.18,-12.18,;-7.84,-11.41,;-7.84,-9.87,;-9.18,-9.1,;-8.78,-7.61,;-9.18,-6.13,;-8.52,-4.79,;-8.92,-3.31,;-8.15,-1.97,;-8.15,-.43,;-6.82,.34,;-6.82,1.88,;-5.48,2.65,;-4.15,1.88,;-2.82,2.65,;-1.48,1.88,;-.15,2.65,;-.15,4.19,;-1.48,4.96,;1.18,4.96,;2.52,4.19,;2.52,2.65,;1.18,1.88,;1.18,.34,;-1.48,.34,;-.15,-.43,;-2.82,-.43,;-2.82,-1.97,;-4.15,.34,;-5.48,-.43,;-10.51,-9.87,;-10.51,-11.41,)|
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