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Assay Detail

CHEMBL924207

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

Binding
Inhibition of MC1 by NADH-DB reductase assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Quinazoline derivatives as MC-I inhibitors: evaluation of myocardial uptake using Positron Emission Tomography in rat and non-human primate.
Purohit A, Benetti R, Hayes M, Guaraldi M, Kagan M, Yalamanchilli P, Su F, Azure M, Mistry M, Yu M, Robinson S, Dischino DD, Casebier D.
Bioorg Med Chem Lett (2007) 17 : 4882 -4885
PubMed 17604167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.31 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243282 FENAZAQUIN 1 8.40
CHEMBL251704 1 7.95
CHEMBL251705 1 7.71
CHEMBL400250 1 7.66
CHEMBL251502 1 7.65
CHEMBL251097 1 7.43
CHEMBL248675 1 6.62
CHEMBL251707 1 6.38
CHEMBL251706 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243282 FENAZAQUIN IC50 = 4.0 nM 8.40
CHEMBL251704 IC50 = 11.3 nM 7.95
CHEMBL251705 IC50 = 19.3 nM 7.71
CHEMBL400250 IC50 = 21.7 nM 7.66
CHEMBL251502 IC50 = 22.4 nM 7.65
CHEMBL251097 IC50 = 37.5 nM 7.43
CHEMBL248675 IC50 = 241.0 nM 6.62
CHEMBL251707 IC50 = 414.0 nM 6.38
CHEMBL251706 IC50 = 1000.0 nM 6.00