Reaction Details
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Fibroblast growth factor receptor 1
Ligand
BDBM4170
Substrate
poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
pH
7±n/a
Temperature
298.15±n/a K
IC50
>50000±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:
BDBM4170
Synonyms:
1,6-naphthyridin-2(1H)-one deriv. 7c | 3-(2,6-Dichlorophenyl)-7-(dimethylamino)-1-methyl-1,6-naphthyridin-2(1H)-one | 3-(2,6-dichlorophenyl)-7-(dimethylamino)-1-methyl-1,2-dihydro-1,6-naphthyridin-2-one
Type:
Small organic molecule
Emp. Form.:
C17H15Cl2N3O
Mol. Mass.:
348.227
SMILES:
CN(C)c1cc2n(C)c(=O)c(cc2cn1)-c1c(Cl)cccc1Cl |(-6.52,-3.49,;-6.52,-1.95,;-7.85,-1.18,;-5.18,-1.18,;-3.85,-1.95,;-2.52,-1.12,;-1.18,-1.89,;-1.18,-3.43,;.15,-1.12,;1.48,-1.89,;.15,.42,;-1.18,1.19,;-2.52,.42,;-3.85,1.13,;-5.18,.36,;1.48,1.19,;1.48,2.73,;.15,3.5,;2.82,3.5,;4.15,2.73,;4.15,1.19,;2.82,.42,;2.82,-1.12,)|
Structure:
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