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Target
Fibroblast growth factor receptor 2
Ligand
BDBM261964
Substrate
n/a
Meas. Tech.
FGFR Enzymatic Assay (pre-incubated for 4 hours)
IC50
20±n/a nM
Citation
 Sokolsky, A; Wu, L; Yao, W Bicyclic heterocycles as FGFR4 inhibitors US Patent  US10251892 Publication Date 4/9/2019
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:
BDBM261964
Synonyms:
3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dimethyl-1H-pyrazol-4-yl)-1- ((5-ethylisoxazol-3-yl)methyl)- 3,4-dihydropyrido[4,3- d]pyrimidin-2(1H)-one | US10251892, Example 64 | US10632126, Example 64 | US11173162, Example 64 | US9708318, 64
Type:
Small organic molecule
Emp. Form.:
C26H26F2N6O4
Mol. Mass.:
524.5192
SMILES:
CCc1cc(CN2C(=O)N(Cc3cnc(cc23)-c2cn(C)nc2C)c2c(F)c(OC)cc(OC)c2F)no1
Structure:
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