Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM4617
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
160±n/a nM
Citation
 Thompson, AM; Connolly, CJ; Hamby, JM; Boushelle, S; Hartl, BG; Amar, AM; Kraker, AJ; Driscoll, DL; Steinkampf, RW; Patmore, SJ; Vincent, PW; Roberts, BJ; Elliott, WL; Klohs, W; Leopold, WR; Showalter, HD; Denny, WA 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. J Med Chem 43:4200-11 (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:
BDBM4617
Synonyms:
1,6-naphthyridine deriv. 19 | 3-tert-butyl-1-{7-[(tert-butylcarbamoyl)amino]-3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-yl}urea | N-(tert-Butyl)-N-[7-(3-tert-butylureido)-3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-yl]urea
Type:
Small organic molecule
Emp. Form.:
C26H34N6O4
Mol. Mass.:
494.586
SMILES:
COc1cc(OC)cc(c1)-c1cc2cnc(NC(=O)NC(C)(C)C)cc2nc1NC(=O)NC(C)(C)C
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