Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM4214
Substrate
poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
180±n/a nM
Citation
 Thompson, AM; Rewcastle, GW; Boushelle, SL; Hartl, BG; Kraker, AJ; Lu, GH; Batley, BL; Panek, RL; Showalter, HD; Denny, WA Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src). J Med Chem 43:3134-47 (2000) [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:
BDBM4214
Synonyms:
4-{[6-(2,6-dichlorophenyl)-8-methyl-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-2-yl]amino}-N,N-diethylbenzamide | Pyrido[2,3-d]pyrimidin-7(8H)-one deriv. 6w
Type:
Small organic molecule
Emp. Form.:
C25H23Cl2N5O2
Mol. Mass.:
496.388
SMILES:
CCN(CC)C(=O)c1ccc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)cc1 |(-13.8,4.21,;-13.8,2.67,;-12.47,1.9,;-12.47,.36,;-13.8,-.41,;-11.11,2.62,;-11.05,4.16,;-9.8,1.8,;-9.86,.26,;-8.55,-.56,;-7.19,.16,;-5.86,-.61,;-4.53,.16,;-4.53,1.7,;-3.19,2.47,;-1.86,1.7,;-.52,2.47,;.81,1.7,;2.14,2.47,;2.14,4.01,;.81,4.78,;3.48,4.78,;4.81,4.01,;4.81,2.47,;3.48,1.7,;3.48,.16,;.81,.16,;2.14,-.61,;-.52,-.61,;-.52,-2.15,;-1.86,.16,;-3.19,-.61,;-7.14,1.7,;-8.44,2.52,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(E:Y)
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
poly (4:1) glutamate-tyrosine. 50 uM ATP and 0.4 uCi [gamma-32P]ATP as co-substrate.
Residue:
3
Sequence:
NA