Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM249440
Substrate
FGFR1 substrate peptide
Meas. Tech.
Kinase HotSpot Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
2694±n/a nM
Comments
extracted
Citation
 Reynolds, D; Hao, M; Wang, J; Prajapati, S; Satoh, T; Selvaraj, A Pyrimidine FGFR4 inhibitors US Patent  US9434697 Publication Date 9/6/2016 
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:
BDBM249440
Synonyms:
US10537571, Compound 161 | US10912774, Compound 161 | US9434697, 161 | US9730931, Compound 161
Type:
Small organic molecule
Emp. Form.:
C29H35Cl2N9O4
Mol. Mass.:
644.552
SMILES:
COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccc(cc3NC(=O)C=C)N3CCN(CCN)CC3)ncn2)c1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
FGFR1 substrate peptide
Synonyms:
n/a
Type:
Protein
Mol. Mass.:
1596.80
Organism:
Artificial Organism
Description:
SEQ ID NO:1
Residue:
14
Sequence:
KKKSPGEYVNIEFG