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Assay Detail

CHEMBL5348490

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

Binding
Inhibition of plasmodium falciparum PK6 incubated for 2 hrs by luciferin-based luminescence assay
84
Total Activities
84
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cdk-related protein kinase 6 (CHEMBL3301558)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH.
Eur J Med Chem (2023) 249 : 115043 -115043
PubMed 36736152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 84 7.78 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5398401 1 9.54
CHEMBL5433238 1 9.36
CHEMBL5418962 1 9.09
CHEMBL5398147 1 9.08
CHEMBL5426653 1 9.00
CHEMBL5395319 1 8.96
CHEMBL5435885 1 8.96
CHEMBL5419731 1 8.92
CHEMBL5413903 1 8.92
CHEMBL5438128 1 8.92
CHEMBL5439780 1 8.89
CHEMBL5393906 1 8.89
CHEMBL5396897 1 8.82
CHEMBL5402319 1 8.80
CHEMBL5427384 1 8.77
CHEMBL5405690 1 8.74
CHEMBL5396095 1 8.74
CHEMBL5404309 1 8.72
CHEMBL5414363 1 8.72
CHEMBL5405119 1 8.72
CHEMBL5431272 1 8.70
CHEMBL5438744 1 8.70
CHEMBL5435130 1 8.68
CHEMBL5414544 1 8.57
CHEMBL5440849 1 8.55
CHEMBL5407751 1 8.51
CHEMBL247228 GW770249X 1 8.28
CHEMBL5407060 1 8.09
CHEMBL5395335 1 8.07
CHEMBL368252 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5398401 IC50 = 0.29 nM 9.54
CHEMBL5433238 IC50 = 0.44 nM 9.36
CHEMBL5418962 IC50 = 0.81 nM 9.09
CHEMBL5398147 IC50 = 0.84 nM 9.08
CHEMBL5426653 IC50 = 1.0 nM 9.00
CHEMBL5395319 IC50 = 1.1 nM 8.96
CHEMBL5435885 IC50 = 1.1 nM 8.96
CHEMBL5419731 IC50 = 1.2 nM 8.92
CHEMBL5413903 IC50 = 1.2 nM 8.92
CHEMBL5438128 IC50 = 1.2 nM 8.92
CHEMBL5439780 IC50 = 1.3 nM 8.89
CHEMBL5393906 IC50 = 1.3 nM 8.89
CHEMBL5396897 IC50 = 1.5 nM 8.82
CHEMBL5402319 IC50 = 1.6 nM 8.80
CHEMBL5427384 IC50 = 1.7 nM 8.77
CHEMBL5405690 IC50 = 1.8 nM 8.74
CHEMBL5396095 IC50 = 1.8 nM 8.74
CHEMBL5404309 IC50 = 1.9 nM 8.72
CHEMBL5414363 IC50 = 1.9 nM 8.72
CHEMBL5405119 IC50 = 1.9 nM 8.72
CHEMBL5431272 IC50 = 2.0 nM 8.70
CHEMBL5438744 IC50 = 2.0 nM 8.70
CHEMBL5435130 IC50 = 2.1 nM 8.68
CHEMBL5414544 IC50 = 2.7 nM 8.57
CHEMBL5440849 IC50 = 2.8 nM 8.55
CHEMBL5407751 IC50 = 3.1 nM 8.51
CHEMBL247228 GW770249X IC50 = 5.3 nM 8.28
CHEMBL5407060 IC50 = 8.1 nM 8.09
CHEMBL5395335 IC50 = 8.5 nM 8.07
CHEMBL368252 IC50 = 9.0 nM 8.05
CHEMBL5415457 IC50 = 10.0 nM 8.00
CHEMBL5417033 IC50 = 12.0 nM 7.92
CHEMBL5400583 IC50 = 12.0 nM 7.92
CHEMBL5417668 IC50 = 13.0 nM 7.89
CHEMBL5414579 IC50 = 13.0 nM 7.89
CHEMBL5421495 IC50 = 14.0 nM 7.85
CHEMBL178455 IC50 = 14.0 nM 7.85
CHEMBL5429163 IC50 = 14.0 nM 7.85
CHEMBL5405467 IC50 = 17.0 nM 7.77
CHEMBL360526 IC50 = 18.0 nM 7.75
CHEMBL5435242 IC50 = 19.0 nM 7.72
CHEMBL5426500 IC50 = 21.0 nM 7.68
CHEMBL5425086 IC50 = 23.0 nM 7.64
CHEMBL5399124 IC50 = 26.0 nM 7.58
CHEMBL5428638 IC50 = 27.0 nM 7.57
CHEMBL5397928 IC50 = 29.0 nM 7.54
CHEMBL5433709 IC50 = 40.0 nM 7.40
CHEMBL5420208 IC50 = 68.0 nM 7.17
CHEMBL5420399 IC50 = 76.0 nM 7.12
CHEMBL5394986 IC50 = 124.0 nM 6.91