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Assay Detail

CHEMBL4340708

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

Binding
Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and measured after 5 mins MALDI TOF MS analysis
35
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Paramecium bursaria Chlorella virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl 4-hydroxylase (CHEMBL4523368)
Type SINGLE PROTEIN
Organism Paramecium bursaria Chlorella virus 1

Publication

Inhibition of a viral prolyl hydroxylase.
Langley GW, Abboud MI, Lohans CT, Schofield CJ.
Bioorg Med Chem (2019) 27 : 2405 -2412
PubMed 30737136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 4.97 5.60
Ki 7 5.48 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3646221 VADADUSTAT 4.0 2 6.55
CHEMBL426560 2 6.15
CHEMBL2338329 ROXADUSTAT 4.0 2 5.97
CHEMBL3646117 1 5.60
CHEMBL316034 2 5.48
CHEMBL4163812 2 5.12
CHEMBL3186774 1 5.07
CHEMBL4475458 1 4.80
CHEMBL3188597 1 4.80
CHEMBL3646118 MOLIDUSTAT 2.0 2 4.79
CHEMBL90852 N-OXALYLGLYCINE 2 4.67
CHEMBL1230640 1 4.33
CHEMBL2164243 1 -
CHEMBL3785984 1 -
CHEMBL4449628 1 -
CHEMBL4540977 1 -
CHEMBL3785164 1 -
CHEMBL347285 1 -
CHEMBL1261 CITRIC ACID 4.0 1 -
CHEMBL390356 ISOCITRIC ACID 1 -
CHEMBL503160 FUMARIC ACID 3.0 1 -
CHEMBL575060 GLUTAMIC ACID 3.0 1 -
CHEMBL1234046 1 -
CHEMBL576 SUCCINIC ACID 3.0 1 -
CHEMBL1615211 1 -
CHEMBL1614745 1 -
CHEMBL1794791 OXALOACETATE 2.0 1 -
CHEMBL1162144 PYRUVATE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3646221 VADADUSTAT Ki = 280.0 nM 6.55
CHEMBL426560 Ki = 710.0 nM 6.15
CHEMBL2338329 ROXADUSTAT Ki = 1070.0 nM 5.97
CHEMBL3646117 IC50 = 2500.0 nM 5.60
CHEMBL316034 Ki = 3280.0 nM 5.48
CHEMBL426560 IC50 = 4500.0 nM 5.35
CHEMBL2338329 ROXADUSTAT IC50 = 5000.0 nM 5.30
CHEMBL316034 IC50 = 5300.0 nM 5.28
CHEMBL4163812 Ki = 7650.0 nM 5.12
CHEMBL3186774 IC50 = 8500.0 nM 5.07
CHEMBL4163812 IC50 = 13400.0 nM 4.87
CHEMBL3188597 IC50 = 15900.0 nM 4.80
CHEMBL4475458 IC50 = 15700.0 nM 4.80
CHEMBL3646118 MOLIDUSTAT Ki = 16050.0 nM 4.79
CHEMBL90852 N-OXALYLGLYCINE IC50 = 21200.0 nM 4.67
CHEMBL3646118 MOLIDUSTAT IC50 = 26800.0 nM 4.57
CHEMBL1230640 IC50 = 47200.0 nM 4.33
CHEMBL90852 N-OXALYLGLYCINE Ki = 48740.0 nM 4.31
CHEMBL503160 FUMARIC ACID IC50 > 1000000.0 nM -
CHEMBL2164243 IC50 > 100000.0 nM -
CHEMBL3785984 IC50 > 100000.0 nM -
CHEMBL4449628 IC50 > 100000.0 nM -
CHEMBL4540977 IC50 > 100000.0 nM -
CHEMBL3785164 IC50 > 100000.0 nM -
CHEMBL3646221 VADADUSTAT IC50 < 1000.0 nM -
CHEMBL1261 CITRIC ACID IC50 = 212600.0 nM -
CHEMBL390356 ISOCITRIC ACID IC50 = 284000.0 nM -
CHEMBL347285 IC50 > 1000000.0 nM -
CHEMBL575060 GLUTAMIC ACID IC50 > 1000000.0 nM -
CHEMBL1234046 IC50 > 1000000.0 nM -
CHEMBL1794791 OXALOACETATE IC50 > 1000000.0 nM -
CHEMBL1162144 PYRUVATE IC50 > 1000000.0 nM -
CHEMBL1614745 IC50 > 500000.0 nM -
CHEMBL1615211 IC50 > 500000.0 nM -
CHEMBL576 SUCCINIC ACID IC50 > 1000000.0 nM -