Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 2
Ligand
BDBM301310
Substrate
n/a
Meas. Tech.
ChEMBL_2188263 (CHEMBL5100345)
IC50
0.400000±n/a nM
Citation
 Shvartsbart, A; Roach, JJ; Witten, MR; Koblish, H; Harris, JJ; Covington, M; Hess, R; Lin, L; Frascella, M; Truong, L; Leffet, L; Conlen, P; Beshad, E; Klabe, R; Katiyar, K; Kaldon, L; Young-Sciame, R; He, X; Petusky, S; Chen, KJ; Horsey, A; Lei, HT; Epling, LB; Deller, MC; Vechorkin, O; Yao, W Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. J Med Chem 65:15433-15442 (2022) [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:
BDBM301310
Synonyms:
3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one | US10131667, Example 126 | US11053246, Example 126 | US11407750, Compound 6 | US9611267, Example 126
Type:
Small organic molecule
Emp. Form.:
C24H27F2N5O4
Mol. Mass.:
487.4991
SMILES:
CCN1C(=O)N(Cc2cnc3[nH]c(CN4CCOCC4)cc3c12)c1c(F)c(OC)cc(OC)c1F
Structure:
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