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Assay Detail

CHEMBL4683364

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

Binding
Inhibition of recombinant His-tagged Plasmodium falciparum 3D7 PI4K expressed in baculovirus infected Sf9 cells using PI:PS as substrate incubated for 1 hr in presence of ATP by ADP-Glo kinase assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum 3D7
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Liang X,Jiang Z,Huang Z,Li F,Chen C,Hu C,Wang W,Hu Z,Liu Q,Wang B,Wang L,Qi Z,Liu J,Jiang L,Liu Q
Eur J Med Chem (2020) 188 : 112012 -112012
PubMed 31911293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 8.34 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4783517 1 9.40
CHEMBL4754454 1 9.30
CHEMBL4752128 1 9.05
CHEMBL4785788 1 8.92
CHEMBL4763185 1 8.92
CHEMBL4758736 1 8.80
CHEMBL3325608 1 8.80
CHEMBL4742705 1 8.66
CHEMBL4753957 1 8.64
CHEMBL4756043 1 8.60
CHEMBL4740991 1 8.35
CHEMBL4204119 1 8.25
CHEMBL4763641 1 8.12
CHEMBL4214320 1 8.11
CHEMBL4777052 1 8.09
CHEMBL4793940 1 8.07
CHEMBL4744808 1 8.06
CHEMBL4784939 1 8.00
CHEMBL4761677 1 7.90
CHEMBL4748442 1 7.88
CHEMBL4740618 1 7.86
CHEMBL4752250 1 7.28
CHEMBL4754047 1 6.84
CHEMBL4764951 1 -
CHEMBL4755281 1 -
CHEMBL4760986 1 -
CHEMBL4760448 1 -
CHEMBL4755814 1 -
CHEMBL4764114 1 -
CHEMBL4799421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4783517 IC50 = 0.4 nM 9.40
CHEMBL4754454 IC50 = 0.5 nM 9.30
CHEMBL4752128 IC50 = 0.9 nM 9.05
CHEMBL4785788 IC50 = 1.2 nM 8.92
CHEMBL4763185 IC50 = 1.2 nM 8.92
CHEMBL4758736 IC50 = 1.6 nM 8.80
CHEMBL3325608 IC50 = 1.6 nM 8.80
CHEMBL4742705 IC50 = 2.2 nM 8.66
CHEMBL4753957 IC50 = 2.3 nM 8.64
CHEMBL4756043 IC50 = 2.5 nM 8.60
CHEMBL4740991 IC50 = 4.5 nM 8.35
CHEMBL4204119 IC50 = 5.6 nM 8.25
CHEMBL4763641 IC50 = 7.5 nM 8.12
CHEMBL4214320 IC50 = 7.7 nM 8.11
CHEMBL4777052 IC50 = 8.1 nM 8.09
CHEMBL4793940 IC50 = 8.5 nM 8.07
CHEMBL4744808 IC50 = 8.8 nM 8.06
CHEMBL4784939 IC50 = 10.0 nM 8.00
CHEMBL4761677 IC50 = 12.7 nM 7.90
CHEMBL4748442 IC50 = 13.2 nM 7.88
CHEMBL4740618 IC50 = 13.8 nM 7.86
CHEMBL4752250 IC50 = 52.6 nM 7.28
CHEMBL4754047 IC50 = 145.1 nM 6.84
CHEMBL4764951 IC50 > 156.0 nM -
CHEMBL4755281 IC50 > 156.0 nM -
CHEMBL4760986 IC50 > 156.0 nM -
CHEMBL4760448 IC50 > 156.0 nM -
CHEMBL4755814 IC50 > 40.0 nM -
CHEMBL4764114 IC50 > 156.0 nM -
CHEMBL4799421 IC50 > 156.0 nM -
CHEMBL4780054 IC50 > 156.0 nM -
CHEMBL4764796 IC50 > 156.0 nM -
CHEMBL4799447 IC50 > 156.0 nM -