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TargetFibroblast growth factor receptor
LigandBDBM4814
Substrate/Competitorpoly(E:Y)
Meas. Tech.Tyrosine Kinase Assay
pH7.5±n/a
Temperature295.15±n/a K
IC50 2900±n/a nM
Citation Sun LLiang CShirazian SZhou YMiller TCui JFukuda JYChu JYNematalla AWang XChen HSistla ALuu TCTang FWei JTang C Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem 46:1116-9 (2003) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Fibroblast growth factor receptor
Name:Fibroblast growth factor receptor
Synonyms:Basic fibroblast growth factor receptor 1 | Basic fibroblast growth factor receptor 1 (FGFR1) | CD_antigen=CD331 | FGFR-1 | FGFR-1 Tyrosine Kinase | FGFR-1, (FL) | FGFR1 | Fibroblast growth factor receptor (FGFR) | Fibroblast growth factor receptor 1 (FGFR-1) | Fibroblast growth factor receptor 1 (FGFR1) | Fms-like tyrosine kinase 2 | bFGF-R | c-fgr
Type:Receptor
Mol. Mass.:91861.70
Organism:Homo sapiens (human)
Description:Recombinant proteins were expressed in Spodoptera frugiperdera 21 (Sf 21) insect cells for the enzyme assay.
Residue:822
Sequence:
MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD
VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD
ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS
SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN
HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI
GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE
ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS
IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL
GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK
HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL
VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG
RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD
KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF
PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
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BDBM4814
NameBDBM4814
Synonyms:CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide | SU11248 | SUNITINIB | SUNITINIB MALATE | US9163010, Sunitinib
TypeSmall organic molecule
Emp. Form.C22H27FN4O2
Mol. Mass.398.4738
SMILESCCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
poly(E:Y)
Name:poly(E:Y)
Synonyms:n/a
Type:Random Polymer
Mol. Mass.:358.43
Organism:n/a
Description:a polyGlu-Tyr peptide (4:1)(Sigma P-0275). 10 uM ATP as co-substrate.
Residue:3
Sequence:
n/a