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Assay Detail

CHEMBL4810143

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

Binding
Inhibition of phosphorylated FGFR2alpha in human KATO III stomach cancer cell line spiked in human whole blood incubated for 4 hrs by ELISA
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type KATO III stomach cancer cell line
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 29 7.70 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870179 1 8.22
CHEMBL4873688 1 8.22
CHEMBL4878157 1 8.17
CHEMBL4848173 1 8.09
CHEMBL4873796 1 8.07
CHEMBL4297522 PEMIGATINIB 4.0 1 7.96
CHEMBL4866175 1 7.96
CHEMBL4857494 1 7.82
CHEMBL4873911 1 7.82
CHEMBL4848945 1 7.80
CHEMBL4862823 1 7.75
CHEMBL4868368 1 7.75
CHEMBL4864630 1 7.75
CHEMBL4853979 1 7.70
CHEMBL4874112 1 7.66
CHEMBL4876826 1 7.62
CHEMBL4851637 1 7.60
CHEMBL4864342 1 7.55
CHEMBL4849808 1 7.54
CHEMBL4847687 1 7.54
CHEMBL4863835 1 7.50
CHEMBL4846809 1 7.48
CHEMBL4856966 1 7.46
CHEMBL4855179 1 7.41
CHEMBL4863146 1 7.19
CHEMBL4863224 1 7.17
CHEMBL4847441 1 7.09
CHEMBL4856613 1 -
CHEMBL4868291 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870179 IC50 = 6.0 nM 8.22
CHEMBL4873688 IC50 = 6.0 nM 8.22
CHEMBL4878157 IC50 = 6.8 nM 8.17
CHEMBL4848173 IC50 = 8.2 nM 8.09
CHEMBL4873796 IC50 = 8.6 nM 8.07
CHEMBL4297522 PEMIGATINIB IC50 = 11.0 nM 7.96
CHEMBL4866175 IC50 = 11.0 nM 7.96
CHEMBL4857494 IC50 = 15.0 nM 7.82
CHEMBL4873911 IC50 = 15.0 nM 7.82
CHEMBL4848945 IC50 = 16.0 nM 7.80
CHEMBL4862823 IC50 = 18.0 nM 7.75
CHEMBL4868368 IC50 = 18.0 nM 7.75
CHEMBL4864630 IC50 = 18.0 nM 7.75
CHEMBL4853979 IC50 = 20.0 nM 7.70
CHEMBL4874112 IC50 = 22.0 nM 7.66
CHEMBL4876826 IC50 = 24.0 nM 7.62
CHEMBL4851637 IC50 = 25.0 nM 7.60
CHEMBL4864342 IC50 = 28.0 nM 7.55
CHEMBL4849808 IC50 = 29.0 nM 7.54
CHEMBL4847687 IC50 = 29.0 nM 7.54
CHEMBL4863835 IC50 = 32.0 nM 7.50
CHEMBL4846809 IC50 = 33.0 nM 7.48
CHEMBL4856966 IC50 = 35.0 nM 7.46
CHEMBL4855179 IC50 = 39.0 nM 7.41
CHEMBL4863146 IC50 = 65.0 nM 7.19
CHEMBL4863224 IC50 = 67.0 nM 7.17
CHEMBL4847441 IC50 = 81.0 nM 7.09
CHEMBL4856613 IC50 - -
CHEMBL4868291 IC50 - -