Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 2
Ligand
BDBM50588768
Substrate
n/a
Meas. Tech.
ChEMBL_2188263 (CHEMBL5100345)
IC50
0.200000±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:
BDBM50588768
Synonyms:
CHEMBL5175256
Type:
Small organic molecule
Emp. Form.:
C23H26N8O2
Mol. Mass.:
449.5234
SMILES:
[2H]C([2H])([2H])NC(=O)c1cncc(c1)-c1cnn2cc(-c3ccn(n3)C(C)C)c(N[C@H]3CCOC3)nc12 |r|
Structure:
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