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Assay Detail

CHEMBL749247

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Binding
Inhibitory activity against NADH oxidase in beef heart mitochondrial complex I.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Mitochondrial complex I; NADH oxidoreductase (CHEMBL614865)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Inhibitory effects on mitochondrial complex I of semisynthetic mono-tetrahydrofuran acetogenin derivatives.
Tormo JR, Gallardo T, Peris E, Bermejo A, Cabedo N, Estornell E, Zafra-Polo MC, Cortes D.
Bioorg Med Chem Lett (2003) 13 : 4101 -4105
PubMed 14592516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.53 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133177 1 9.15
CHEMBL134189 1 9.10
CHEMBL131461 1 8.72
CHEMBL439797 1 8.64
CHEMBL133015 1 8.57
CHEMBL131124 1 8.48
CHEMBL132607 1 8.44
CHEMBL429023 ROTENONE 1 8.29
CHEMBL131462 1 8.24
CHEMBL131506 1 7.66
CHEMBL133297 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133177 IC50 = 0.7 nM 9.15
CHEMBL134189 IC50 = 0.8 nM 9.10
CHEMBL131461 IC50 = 1.9 nM 8.72
CHEMBL439797 IC50 = 2.3 nM 8.64
CHEMBL133015 IC50 = 2.7 nM 8.57
CHEMBL131124 IC50 = 3.3 nM 8.48
CHEMBL132607 IC50 = 3.6 nM 8.44
CHEMBL429023 ROTENONE IC50 = 5.1 nM 8.29
CHEMBL131462 IC50 = 5.8 nM 8.24
CHEMBL131506 IC50 = 21.8 nM 7.66
CHEMBL133297 IC50 > 150.0 nM -