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Assay Detail

CHEMBL4810138

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human FGFR2 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 2 (CHEMBL4142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
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.
J Med Chem (2021) 64 : 10666 -10679
PubMed 34269576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.77 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870179 1 9.82
CHEMBL4862823 1 9.52
CHEMBL4863146 1 9.00
CHEMBL4847441 1 8.85
CHEMBL4863224 1 8.85
CHEMBL4856613 1 8.36
CHEMBL4868291 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870179 IC50 = 0.15 nM 9.82
CHEMBL4862823 IC50 = 0.3 nM 9.52
CHEMBL4863146 IC50 = 1.0 nM 9.00
CHEMBL4847441 IC50 = 1.4 nM 8.85
CHEMBL4863224 IC50 = 1.4 nM 8.85
CHEMBL4856613 IC50 = 4.4 nM 8.36
CHEMBL4868291 IC50 = 97.0 nM 7.01