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Assay Detail

CHEMBL678318

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

Binding
Inhibitory concentration towards rat mitochondrial F1F0 ATP hydrolase using a pyruvate kinase / lactate dehydrogenase system
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

Mitochondrial complex V; ATP synthase (CHEMBL612444)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
Atwal KS, Wang P, Rogers WL, Sleph P, Monshizadegan H, Ferrara FN, Traeger S, Green DW, Grover GJ.
J Med Chem (2004) 47 : 1081 -1084
PubMed 14971888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.79 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11859 1 6.62
CHEMBL11502 1 6.32
CHEMBL11594 BMS-191095 1 6.32
CHEMBL273271 1 5.85
CHEMBL428891 1 5.70
CHEMBL273900 1 5.38
CHEMBL274443 1 4.35
CHEMBL429014 1 -
CHEMBL11802 1 -
CHEMBL268271 1 -
CHEMBL11458 1 -
CHEMBL11392 1 -
CHEMBL472 GLYBURIDE 4.0 1 -
CHEMBL49035 CROMAKALIM 2.0 1 -
CHEMBL11183 1 -
CHEMBL2052011 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11859 IC50 = 240.0 nM 6.62
CHEMBL11502 IC50 = 480.0 nM 6.32
CHEMBL11594 BMS-191095 IC50 = 480.0 nM 6.32
CHEMBL273271 IC50 = 1400.0 nM 5.85
CHEMBL428891 IC50 = 2000.0 nM 5.70
CHEMBL273900 IC50 = 4200.0 nM 5.38
CHEMBL274443 IC50 = 45000.0 nM 4.35
CHEMBL429014 IC50 > 100000.0 nM -
CHEMBL11802 IC50 > 100000.0 nM -
CHEMBL268271 IC50 > 100000.0 nM -
CHEMBL11458 IC50 > 100000.0 nM -
CHEMBL11392 IC50 > 30000.0 nM -
CHEMBL472 GLYBURIDE IC50 > 100000.0 nM -
CHEMBL49035 CROMAKALIM IC50 > 100000.0 nM -
CHEMBL11183 IC50 > 100000.0 nM -
CHEMBL2052011 IC50 = 470000.0 nM -