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Target
Fibroblast growth factor receptor 2
Ligand
BDBM161389
Substrate
n/a
Meas. Tech.
ChEMBL_2296007
IC50
1.000000±n/a nM
Citation
 Ito, S; Otsuki, S; Ohsawa, H; Hirano, A; Kazuno, H; Yamashita, S; Egami, K; Shibata, Y; Yamamiya, I; Yamashita, F; Kodama, Y; Funabashi, K; Kazuno, H; Komori, T; Suzuki, S; Sootome, H; Hirai, H; Sagara, T Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use. ACS Med Chem Lett 14:396-404 (2023) [PubMed] 
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:
BDBM161389
Synonyms:
US10124003, Ref. Ex. Compound 3 | US10835536, Ex. Comp 2 | US10894048, Ex Comp 2 | US9108973, 2
Type:
Small organic molecule
Emp. Form.:
C22H22N6O3
Mol. Mass.:
418.4485
SMILES:
COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
Structure:
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