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Assay Detail

CHEMBL4810140

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

ADMET
Inhibition of human recombinant N-terminal His6-tagged VEGFR2 expressed in baculovirus infected Sf21insect cells using biotin-labeled EQEDEPEGDYFEWLE peptide as substrate incubated for 20 mins in presence of ATP by plate reader assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
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 9 6.69 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870179 1 7.62
CHEMBL4862823 1 7.40
CHEMBL4863224 1 7.04
CHEMBL4847441 1 6.88
CHEMBL4863146 1 6.79
CHEMBL4856613 1 6.34
CHEMBL4861534 1 5.78
CHEMBL4862283 1 5.69
CHEMBL4868291 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870179 IC50 = 24.0 nM 7.62
CHEMBL4862823 IC50 = 40.0 nM 7.40
CHEMBL4863224 IC50 = 92.0 nM 7.04
CHEMBL4847441 IC50 = 131.0 nM 6.88
CHEMBL4863146 IC50 = 162.0 nM 6.79
CHEMBL4856613 IC50 = 452.0 nM 6.34
CHEMBL4861534 IC50 = 1677.0 nM 5.78
CHEMBL4862283 IC50 = 2058.0 nM 5.69
CHEMBL4868291 IC50 > 2000.0 nM -