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Assay Detail

CHEMBL948046

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Binding
Inhibition of NADH-ubiquinone oxidoreductase assessed as NADH oxidase activity in bovine heart submitochondrial particles
17
Total Activities
17
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

Iromycins from Streptomyces sp. and from synthesis: new inhibitors of the mitochondrial electron transport chain.
Surup F, Shojaei H, von Zezschwitz P, Kunze B, Grond S.
Bioorg Med Chem (2008) 16 : 1738 -1746
PubMed 18054490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.87 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272733 PIERICIDIN A 1 8.30
CHEMBL258096 IROMYCIN S 1 6.74
CHEMBL270860 IROMYCIN A 1 6.34
CHEMBL272324 IROMYCIN M 1 6.00
CHEMBL270644 IROMYCIN AH 1 5.66
CHEMBL270201 IROMYCIN AM 1 5.55
CHEMBL257864 IROMYCIN C 1 5.45
CHEMBL256862 IROMYCIN MO 1 5.07
CHEMBL258094 IROMYCIN SO 1 4.82
CHEMBL269802 IROMYCIN B 1 4.75
CHEMBL272356 IROMYCIN E 1 -
CHEMBL272059 IROMYCIN F 1 -
CHEMBL256056 IROMYCIN BM 1 -
CHEMBL256051 IROMYCIN AA 1 -
CHEMBL256863 IROMYCIN BA 1 -
CHEMBL258095 IROMYCIN AO 1 -
CHEMBL272780 IROMYCIN D 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272733 PIERICIDIN A IC50 = 5.0 nM 8.30
CHEMBL258096 IROMYCIN S IC50 = 183.0 nM 6.74
CHEMBL270860 IROMYCIN A IC50 = 461.0 nM 6.34
CHEMBL272324 IROMYCIN M IC50 = 1010.0 nM 6.00
CHEMBL270644 IROMYCIN AH IC50 = 2210.0 nM 5.66
CHEMBL270201 IROMYCIN AM IC50 = 2800.0 nM 5.55
CHEMBL257864 IROMYCIN C IC50 = 3520.0 nM 5.45
CHEMBL256862 IROMYCIN MO IC50 = 8550.0 nM 5.07
CHEMBL258094 IROMYCIN SO IC50 = 15100.0 nM 4.82
CHEMBL269802 IROMYCIN B IC50 = 17800.0 nM 4.75
CHEMBL272356 IROMYCIN E IC50 > 25300.0 nM -
CHEMBL272059 IROMYCIN F IC50 > 25300.0 nM -
CHEMBL256056 IROMYCIN BM IC50 > 24300.0 nM -
CHEMBL256051 IROMYCIN AA IC50 > 23400.0 nM -
CHEMBL256863 IROMYCIN BA IC50 > 22400.0 nM -
CHEMBL258095 IROMYCIN AO IC50 > 26600.0 nM -
CHEMBL272780 IROMYCIN D IC50 > 26500.0 nM -