Target
Fibroblast growth factor receptor 1
Ligand
BDBM287543
Substrate
n/a
Meas. Tech.
Caliper-Based Kinase Assay
Temperature
298.15±n/a K
IC50
6.90±n/a nM
Comments
extracted
Citation
 Verner, EBrameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US9567334 Publication Date 2/14/2017 
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:
BDBM287543
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((3-(pyrrolidin-1-yl)propyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 99 | US11078199, Cpd 99 | US9567334, Example 99
Type:
Small organic molecule
Emp. Form.:
C30H36Cl2N6O5
Mol. Mass.:
631.55
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCCN3CCCC3)nc2n(CCOC2CN(C2)C(=O)C=C)c1=O |(6.24,7.86,;4.91,7.09,;4.91,5.55,;6.24,4.78,;6.24,3.24,;7.58,2.47,;8.91,3.24,;4.91,2.47,;4.91,.93,;3.58,3.24,;3.58,4.78,;2.24,5.55,;2.24,2.47,;.91,3.24,;-.43,2.47,;-1.76,3.24,;-3.09,2.47,;-3.09,.93,;-4.43,.16,;-4.43,-1.38,;-5.76,-2.15,;-5.76,-3.69,;-7.09,-4.46,;-8.56,-3.98,;-9.46,-5.23,;-8.56,-6.48,;-7.09,-6,;-1.76,.16,;-.43,.93,;.91,.16,;.91,-1.38,;2.24,-2.15,;2.24,-3.69,;3.58,-4.46,;3.97,-5.95,;5.46,-5.55,;5.06,-4.06,;6.8,-6.32,;6.8,-7.86,;8.13,-5.55,;9.46,-6.32,;2.24,.93,;3.58,.16,)|
Structure:
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