Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 3
Ligand
BDBM301217
Substrate
n/a
Meas. Tech.
ChEMBL_2101743 (CHEMBL4810139)
IC50
0.270000±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
More Info.:
Target
Name:
Fibroblast growth factor receptor 3
Synonyms:
CD_antigen: CD333 | FGFR-3 | FGFR3 | FGFR3_HUMAN | Fibroblast growth factor receptor | Fibroblast growth factor receptor 3 (FGFR3) | JTK4
Type:
Protein
Mol. Mass.:
87699.57
Organism:
Homo sapiens (Human)
Description:
P22607
Residue:
806
Sequence:
MGAPACALALCVAVAIVAGASSESLGTEQRVVGRAAEVPGPEPGQQEQLVFGSGDAVELSCPPPGGGPMGPTVWVKDGTGLVPSERVLVGPQRLQVLNASHEDSGAYSCRQRLTQRVLCHFSVRVTDAPSSGDDEDGEDEAEDTGVDTGAPYWTRPERMDKKLLAVPAANTVRFRCPAAGNPTPSISWLKNGREFRGEHRIGGIKLRHQQWSLVMESVVPSDRGNYTCVVENKFGSIRQTYTLDVLERSPHRPILQAGLPANQTAVLGSDVEFHCKVYSDAQPHIQWLKHVEVNGSKVGPDGTPYVTVLKTAGANTTDKELEVLSLHNVTFEDAGEYTCLAGNSIGFSHHSAWLVVLPAEEELVEADEAGSVYAGILSYGVGFFLFILVVAAVTLCRLRSPPKKGLGSPTVHKISRFPLKRQVSLESNASMSSNTPLVRIARLSSGEGPTLANVSELELPADPKWELSRARLTLGKPLGEGCFGQVVMAEAIGIDKDRAAKPVTVAVKMLKDDATDKDLSDLVSEMEMMKMIGKHKNIINLLGACTQGGPLYVLVEYAAKGNLREFLRARRPPGLDYSFDTCKPPEEQLTFKDLVSCAYQVARGMEYLASQKCIHRDLAARNVLVTEDNVMKIADFGLARDVHNLDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLLWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTHDLYMIMRECWHAAPSQRPTFKQLVEDLDRVLTVTSTDEYLDLSAPFEQYSPGGQDTPSSSSSGDDSVFAHDLLPPAPPSSGGSRT
Inhibitor
Name:
BDBM301217
Synonyms:
3-(2,6-Difluoro-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 33 | US11053246, Example 33 | US9611267, Example 33
Type:
Small organic molecule
Emp. Form.:
C18H16F2N4O3
Mol. Mass.:
374.3414
SMILES:
COc1cc(OC)c(F)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F