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Target
Fibroblast growth factor receptor 2
Ligand
BDBM301220
Substrate
n/a
Meas. Tech.
ChEMBL_2101742 (CHEMBL4810138)
IC50
0.300000±n/a nM
Citation
 Wu, L; Zhang, C; He, C; Qian, D; Lu, L; Sun, Y; Xu, M; Zhuo, J; Liu, PCC; Klabe, R; Wynn, R; Covington, M; Gallagher, K; Leffet, L; Bowman, K; Diamond, S; Koblish, H; Zhang, Y; Soloviev, M; Hollis, G; Burn, TC; Scherle, P; Yeleswaram, S; Huber, R; Yao, W Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. J Med Chem 64:10666-10679 (2021) [PubMed]  Article 
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:
BDBM301220
Synonyms:
3-(2-Chloro-6-fluoro-3,5-dimethoxyphenyl)-1-methyl-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one | US10131667, Example 36 | US11053246, Example 36 | US9611267, Example 36
Type:
Small organic molecule
Emp. Form.:
C18H16ClFN4O3
Mol. Mass.:
390.796
SMILES:
COc1cc(OC)c(Cl)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F
Structure:
Search PDB for entries with ligand similarity: