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Assay Detail

CHEMBL5111458

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

Binding
Inhibition of human GST tagged PIKFYVE (1493 to end residues) expressed in baculovirus-infected Sf9 cells using PI(3)P:PS as substrate incubated for 60 mins in presence of ATP by ADP-Glo assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

1-phosphatidylinositol 3-phosphate 5-kinase (CHEMBL1938222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.
Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M, McPherson PS, Moorman NJ, Axtman AD.
J Med Chem (2022) 65 : 12860 -12882
PubMed 36111834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.69 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178735 1 9.09
CHEMBL5189479 1 8.74
CHEMBL5193848 1 8.72
CHEMBL2334586 1 8.66
CHEMBL4297643 APILIMOD 2.0 1 8.47
CHEMBL4303292 1 8.43
CHEMBL5181163 1 8.21
CHEMBL5198944 1 8.21
CHEMBL5174830 1 8.16
CHEMBL5207387 1 8.09
CHEMBL5171753 1 8.03
CHEMBL5190524 1 7.66
CHEMBL5188159 1 7.58
CHEMBL5200109 1 7.47
CHEMBL5202422 1 7.21
CHEMBL5190724 1 7.12
CHEMBL5192827 1 7.11
CHEMBL5184182 1 6.85
CHEMBL5203403 1 6.54
CHEMBL5190455 1 6.37
CHEMBL5204874 1 6.24
CHEMBL5199026 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178735 IC50 = 0.82 nM 9.09
CHEMBL5189479 IC50 = 1.8 nM 8.74
CHEMBL5193848 IC50 = 1.9 nM 8.72
CHEMBL2334586 IC50 = 2.2 nM 8.66
CHEMBL4297643 APILIMOD IC50 = 3.4 nM 8.47
CHEMBL4303292 IC50 = 3.7 nM 8.43
CHEMBL5181163 IC50 = 6.1 nM 8.21
CHEMBL5198944 IC50 = 6.2 nM 8.21
CHEMBL5174830 IC50 = 6.9 nM 8.16
CHEMBL5207387 IC50 = 8.2 nM 8.09
CHEMBL5171753 IC50 = 9.3 nM 8.03
CHEMBL5190524 IC50 = 22.0 nM 7.66
CHEMBL5188159 IC50 = 26.0 nM 7.58
CHEMBL5200109 IC50 = 34.0 nM 7.47
CHEMBL5202422 IC50 = 61.0 nM 7.21
CHEMBL5190724 IC50 = 75.0 nM 7.12
CHEMBL5192827 IC50 = 77.0 nM 7.11
CHEMBL5184182 IC50 = 140.0 nM 6.85
CHEMBL5203403 IC50 = 290.0 nM 6.54
CHEMBL5190455 IC50 = 430.0 nM 6.37
CHEMBL5204874 IC50 = 580.0 nM 6.24
CHEMBL5199026 IC50 = 720.0 nM 6.14