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Assay Detail

CHEMBL959146

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

Binding
Inhibition of mitochondrial complex 1 in bovine heart mitochondria assessed as effect on rate of NADH oxidation
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Heart
Subcellular Mitochondria
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological evaluation of pyridazinone analogues as potential cardiac positron emission tomography tracers.
Purohit A, Radeke H, Azure M, Hanson K, Benetti R, Su F, Yalamanchili P, Yu M, Hayes M, Guaraldi M, Kagan M, Robinson S, Casebier D.
J Med Chem (2008) 51 : 2954 -2970
PubMed 18422306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.33 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225963 PYRIDABEN 1 8.10
CHEMBL493613 1 8.10
CHEMBL243937 1 8.05
CHEMBL493612 1 8.00
CHEMBL494622 FLURPIRIDAZ 4.0 1 7.96
CHEMBL468381 1 7.96
CHEMBL493593 1 7.82
CHEMBL429023 ROTENONE 1 7.80
CHEMBL523353 1 7.80
CHEMBL494755 1 7.77
CHEMBL494640 1 7.68
CHEMBL494756 1 7.57
CHEMBL494623 1 7.55
CHEMBL522356 1 7.51
CHEMBL505265 1 7.33
CHEMBL356903 1 7.28
CHEMBL493423 1 7.22
CHEMBL500046 1 7.19
CHEMBL243282 FENAZAQUIN 1 7.05
CHEMBL521999 1 6.66
CHEMBL524041 1 6.60
CHEMBL445251 1 6.55
CHEMBL494754 1 6.15
CHEMBL523878 1 6.07
CHEMBL493406 1 5.40
CHEMBL493629 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225963 PYRIDABEN IC50 = 8.0 nM 8.10
CHEMBL493613 IC50 = 8.0 nM 8.10
CHEMBL243937 IC50 = 9.0 nM 8.05
CHEMBL493612 IC50 = 10.0 nM 8.00
CHEMBL494622 FLURPIRIDAZ IC50 = 11.0 nM 7.96
CHEMBL468381 IC50 = 11.0 nM 7.96
CHEMBL493593 IC50 = 15.0 nM 7.82
CHEMBL429023 ROTENONE IC50 = 16.0 nM 7.80
CHEMBL523353 IC50 = 16.0 nM 7.80
CHEMBL494755 IC50 = 17.0 nM 7.77
CHEMBL494640 IC50 = 21.0 nM 7.68
CHEMBL494756 IC50 = 27.0 nM 7.57
CHEMBL494623 IC50 = 28.0 nM 7.55
CHEMBL522356 IC50 = 31.0 nM 7.51
CHEMBL505265 IC50 = 47.0 nM 7.33
CHEMBL356903 IC50 = 52.0 nM 7.28
CHEMBL493423 IC50 = 60.0 nM 7.22
CHEMBL500046 IC50 = 64.0 nM 7.19
CHEMBL243282 FENAZAQUIN IC50 = 90.0 nM 7.05
CHEMBL521999 IC50 = 221.0 nM 6.66
CHEMBL524041 IC50 = 250.0 nM 6.60
CHEMBL445251 IC50 = 279.0 nM 6.55
CHEMBL494754 IC50 = 711.0 nM 6.15
CHEMBL523878 IC50 = 850.0 nM 6.07
CHEMBL493406 IC50 = 4000.0 nM 5.40
CHEMBL493629 IC50 > 4000.0 nM -