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Assay Detail

CHEMBL5111459

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Binding
Inhibition of PIKFYVE in HEK293 cells by NanoBRET assay
ChEMBL ↗
49
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 49 6.80 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297643 APILIMOD 2.0 2 9.51
CHEMBL4303292 — — 2 8.92
CHEMBL5174830 — — 2 8.40
CHEMBL5171359 — — 1 8.39
CHEMBL5193848 — — 1 8.02
CHEMBL5171753 — — 2 7.94
CHEMBL5189479 — — 2 7.90
CHEMBL2334586 — — 1 7.85
CHEMBL5181163 — — 1 7.68
CHEMBL5185288 — — 1 7.40
CHEMBL5190153 — — 1 7.34
CHEMBL2178735 — — 2 7.13
CHEMBL5187698 — — 1 6.91
CHEMBL5194568 — — 1 6.66
CHEMBL5194935 — — 1 6.54
CHEMBL5194053 — — 1 6.52
CHEMBL5198944 — — 1 6.50
CHEMBL5207387 — — 2 6.42
CHEMBL5190455 — — 1 6.17
CHEMBL5190724 — — 2 6.16
CHEMBL5190524 — — 2 6.05
CHEMBL5171207 — — 2 5.93
CHEMBL5188159 — — 2 5.81
CHEMBL5184182 — — 1 5.80
CHEMBL5191449 — — 1 5.67
CHEMBL5202422 — — 2 5.61
CHEMBL5180067 — — 1 5.59
CHEMBL5204313 — — 1 5.53
CHEMBL5200109 — — 2 5.30
CHEMBL5204874 — — 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297643 APILIMOD IC50 = 0.309 nM 9.51
CHEMBL4297643 APILIMOD IC50 = 0.312 nM 9.51
CHEMBL4303292 — IC50 = 1.202 nM 8.92
CHEMBL4303292 — IC50 = 1.19 nM 8.92
CHEMBL5174830 — IC50 = 4.01 nM 8.40
CHEMBL5174830 — IC50 = 3.981 nM 8.40
CHEMBL5171359 — IC50 = 4.05 nM 8.39
CHEMBL5193848 — IC50 = 9.65 nM 8.02
CHEMBL5171753 — IC50 = 11.48 nM 7.94
CHEMBL5171753 — IC50 = 11.4 nM 7.94
CHEMBL5189479 — IC50 = 12.59 nM 7.90
CHEMBL5189479 — IC50 = 12.7 nM 7.90
CHEMBL2334586 — IC50 = 14.1 nM 7.85
CHEMBL5181163 — IC50 = 21.1 nM 7.68
CHEMBL5185288 — IC50 = 40.0 nM 7.40
CHEMBL5190153 — IC50 = 45.7 nM 7.34
CHEMBL2178735 — IC50 = 74.13 nM 7.13
CHEMBL2178735 — IC50 = 73.5 nM 7.13
CHEMBL5187698 — IC50 = 123.0 nM 6.91
CHEMBL5194568 — IC50 = 220.0 nM 6.66
CHEMBL5194935 — IC50 = 290.0 nM 6.54
CHEMBL5194053 — IC50 = 300.0 nM 6.52
CHEMBL5198944 — IC50 = 314.0 nM 6.50
CHEMBL5207387 — IC50 = 380.0 nM 6.42
CHEMBL5207387 — IC50 = 380.19 nM 6.42
CHEMBL5190455 — IC50 = 683.0 nM 6.17
CHEMBL5190724 — IC50 = 700.0 nM 6.16
CHEMBL5190724 — IC50 = 707.95 nM 6.15
CHEMBL5190524 — IC50 = 891.25 nM 6.05
CHEMBL5190524 — IC50 = 885.0 nM 6.05
CHEMBL5171207 — IC50 = 1170.0 nM 5.93
CHEMBL5171207 — IC50 = 1174.9 nM 5.93
CHEMBL5188159 — IC50 = 1548.82 nM 5.81
CHEMBL5188159 — IC50 = 1560.0 nM 5.81
CHEMBL5184182 — IC50 = 1600.0 nM 5.80
CHEMBL5191449 — IC50 = 2160.0 nM 5.67
CHEMBL5202422 — IC50 = 2450.0 nM 5.61
CHEMBL5202422 — IC50 = 2454.71 nM 5.61
CHEMBL5180067 — IC50 = 2560.0 nM 5.59
CHEMBL5204313 — IC50 = 2980.0 nM 5.53
CHEMBL5200109 — IC50 = 4970.0 nM 5.30
CHEMBL5200109 — IC50 = 5011.87 nM 5.30
CHEMBL5204874 — IC50 = 5290.0 nM 5.28
CHEMBL5199026 — IC50 = 10000.0 nM 5.00
CHEMBL5192827 — IC50 = 10000.0 nM 5.00
CHEMBL5199026 — IC50 > 10000.0 nM -
CHEMBL5203403 — IC50 > 10000.0 nM -
CHEMBL5177428 — IC50 > 10000.0 nM -
CHEMBL5192827 — IC50 > 10000.0 nM -