Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 2
Ligand
BDBM287011
Substrate
n/a
Meas. Tech.
Inhibition of FGFR2-Dependent Cell Growth
IC50
16.1±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US10294223 Publication Date 5/21/2019 
Target
Name:
Fibroblast growth factor receptor 2
Synonyms:
BEK | CD_antigen=CD332 | FGFR-2 | FGFR-2 Tyrosine Kinase | FGFR2 | FGFR2_HUMAN | Fibroblast growth factor receptor 2 (FGFR2) | Fibroblast growth factor receptor 2 precursor | KGFR | KSAM | Keratinocyte growth factor receptor | Keratinocyte growth factor receptor 2 | VEGF-receptor 2 and Fibroblast growth factor receptor 2
Type:
Enzyme
Mol. Mass.:
92015.45
Organism:
Homo sapiens (Human)
Description:
P21802
Residue:
821
Sequence:
MVSWGRFICLVVVTMATLSLARPSFSLVEDTTLEPEEPPTKYQISQPEVYVAAPGESLEVRCLLKDAAVISWTKDGVHLGPNNRTVLIGEYLQIKGATPRDSGLYACTASRTVDSETWYFMVNVTDAISSGDDEDDTDGAEDFVSENSNNKRAPYWTNTEKMEKRLHAVPAANTVKFRCPAGGNPMPTMRWLKNGKEFKQEHRIGGYKVRNQHWSLIMESVVPSDKGNYTCVVENEYGSINHTYHLDVVERSPHRPILQAGLPANASTVVGGDVEFVCKVYSDAQPHIQWIKHVEKNGSKYGPDGLPYLKVLKAAGVNTTDKEIEVLYIRNVTFEDAGEYTCLAGNSIGISFHSAWLTVLPAPGREKEITASPDYLEIAIYCIGVFLIACMVVTVILCRMKNTTKKPDFSSQPAVHKLTKRIPLRRQVTVSAESSSSMNSNTPLVRITTRLSSTADTPMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEEYLDLSQPLEQYSPSYPDTRSSCSSGDDSVFSPDPMPYEPCLPQYPHINGSVKT
  
Inhibitor
Name:
BDBM287011
Synonyms:
8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((2,2,2-trifluoroethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 55 | US11078199, Cpd 55 | US9567334, Example 55 | US9815834, Compound 55
Type:
Small organic molecule
Emp. Form.:
C27H29Cl2F3N6O4
Mol. Mass.:
629.458
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCC(F)(F)F)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O |(2.67,8.47,;4,7.7,;4,6.16,;5.33,5.39,;5.33,3.85,;6.67,3.08,;8,3.85,;4,3.08,;4,1.54,;2.67,3.85,;2.67,5.39,;1.33,6.16,;1.33,3.08,;,3.85,;-1.33,3.08,;-2.67,3.85,;-4,3.08,;-4,1.54,;-5.33,.77,;-5.33,-.77,;-6.67,-1.54,;-6.67,-3.08,;-8,-.77,;-8,-2.31,;-2.67,.77,;-1.33,1.54,;,.77,;,-.77,;1.33,-1.54,;1.33,-3.08,;2.67,-3.85,;2.67,-5.39,;4,-6.16,;5.33,-5.39,;5.33,-3.85,;4,-3.08,;6.67,-6.16,;8,-5.39,;6.67,-7.7,;8,-8.47,;1.33,1.54,;2.67,.77,)|
Structure:
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