Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 2
Ligand
BDBM287027
Substrate
n/a
Meas. Tech.
Inhibition of FGFR2-Dependent Cell Growth
IC50
8.60±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:
BDBM287027
Synonyms:
(S)-8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((tetrahydrofuran-3-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 58 | US11078199, Cpd 58 | US9567334, Example 58 | US9815834, Compound 58
Type:
Small organic molecule
Emp. Form.:
C29H34Cl2N6O5
Mol. Mass.:
617.523
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@H]3CCOC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O |r,wU:19.19,(1.96,8.47,;3.29,7.7,;3.29,6.16,;4.62,5.39,;4.62,3.85,;5.96,3.08,;7.29,3.85,;3.29,3.08,;3.29,1.54,;1.96,3.85,;1.96,5.39,;.62,6.16,;.62,3.08,;-.71,3.85,;-2.04,3.08,;-3.38,3.85,;-4.71,3.08,;-4.71,1.54,;-6.05,.77,;-6.05,-.77,;-4.8,-1.68,;-5.28,-3.14,;-6.82,-3.14,;-7.29,-1.68,;-3.38,.77,;-2.04,1.54,;-.71,.77,;-.71,-.77,;.62,-1.54,;.62,-3.08,;1.96,-3.85,;1.96,-5.39,;3.29,-6.16,;4.62,-5.39,;4.62,-3.85,;3.29,-3.08,;5.96,-6.16,;7.29,-5.39,;5.96,-7.7,;7.29,-8.47,;.62,1.54,;1.96,.77,)|
Structure:
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