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Assay Detail

CHEMBL3065755

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

Binding
Inhibition of Aquifex aeolicus IspH expressed in Escherichia coli BL21 (DE3) using HMBPP substrate
23
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aquifex aeolicus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

4-hydroxy-3-methylbut-2-enyl diphosphate reductase (CHEMBL2242741)
Type SINGLE PROTEIN
Organism Aquifex aeolicus (strain VF5)

Publication

Inhibition of the Fe(4)S(4)-cluster-containing protein IspH (LytB): electron paramagnetic resonance, metallacycles, and mechanisms.
Wang K, Wang W, No JH, Zhang Y, Zhang Y, Oldfield E.
J Am Chem Soc (2010) 132 : 6719 -6727
PubMed 20426416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 4.90 6.35
Ki 2 6.57 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2251810 BUT-3-YNYL DIPHOSPHATE 2 7.22
CHEMBL2251821 PYRIDIN-3-YL-ETHYL-DIPHOSPHATE 2 5.92
CHEMBL2251811 PENT-4-YNYL DIPHOSPHATE 1 5.19
CHEMBL2251809 PROP-2-YNYL DIPHOSPHATE 1 5.17
CHEMBL2251812 4-HYDROXYBUT-2-YNYL DIPHOSPHATE 1 4.58
CHEMBL2251817 1 4.42
CHEMBL2251814 2-CYANOETHYL DIPHOSPHATE 1 4.28
CHEMBL55557 1 4.17
CHEMBL2251819 (PYRIDIN-2-YL)-METHYL-DIPHOSPHATE 1 -
CHEMBL2251818 (PYRIDIN-4-YL)-METHYL-DIPHOSPHATE 1 -
CHEMBL2251816 1 -
CHEMBL98110 1 -
CHEMBL294192 1 -
CHEMBL434024 1 -
CHEMBL923 RISEDRONIC ACID 4.0 1 -
CHEMBL99553 1 -
CHEMBL193356 1 -
CHEMBL2251815 1 -
CHEMBL2251813 CYANOMETHYL DIPHOSPHATE 1 -
CHEMBL2251820 1 -
CHEMBL2251822 PYRIDIN-3-YL-PROPYL-DIPHOSPHATE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2251810 BUT-3-YNYL DIPHOSPHATE Ki = 60.0 nM 7.22
CHEMBL2251810 BUT-3-YNYL DIPHOSPHATE IC50 = 450.0 nM 6.35
CHEMBL2251821 PYRIDIN-3-YL-ETHYL-DIPHOSPHATE Ki = 1200.0 nM 5.92
CHEMBL2251811 PENT-4-YNYL DIPHOSPHATE IC50 = 6500.0 nM 5.19
CHEMBL2251809 PROP-2-YNYL DIPHOSPHATE IC50 = 6700.0 nM 5.17
CHEMBL2251821 PYRIDIN-3-YL-ETHYL-DIPHOSPHATE IC50 = 9100.0 nM 5.04
CHEMBL2251812 4-HYDROXYBUT-2-YNYL DIPHOSPHATE IC50 = 26000.0 nM 4.58
CHEMBL2251817 IC50 = 38000.0 nM 4.42
CHEMBL2251814 2-CYANOETHYL DIPHOSPHATE IC50 = 53000.0 nM 4.28
CHEMBL55557 IC50 = 67000.0 nM 4.17
CHEMBL2251819 (PYRIDIN-2-YL)-METHYL-DIPHOSPHATE IC50 = 1200000.0 nM -
CHEMBL2251818 (PYRIDIN-4-YL)-METHYL-DIPHOSPHATE IC50 = 149000.0 nM -
CHEMBL2251816 IC50 > 1000000.0 nM -
CHEMBL98110 IC50 > 1000000.0 nM -
CHEMBL294192 IC50 > 1000000.0 nM -
CHEMBL434024 IC50 = 485000.0 nM -
CHEMBL2251820 IC50 = 3700000.0 nM -
CHEMBL99553 IC50 > 1000000.0 nM -
CHEMBL193356 IC50 = 540000.0 nM -
CHEMBL2251815 IC50 > 1000000.0 nM -
CHEMBL2251813 CYANOMETHYL DIPHOSPHATE IC50 = 245000.0 nM -
CHEMBL2251822 PYRIDIN-3-YL-PROPYL-DIPHOSPHATE IC50 = 463000.0 nM -
CHEMBL923 RISEDRONIC ACID IC50 > 1000000.0 nM -