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Assay Detail

CHEMBL4271952

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

Functional
Cytotoxicity against human NCI-H1650 cells assessed as decrease in cell viability after 72 hrs by MTT assay
17
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1650
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H1650 (CHEMBL1075518)
Type CELL-LINE
Organism Homo sapiens

Publication

Rational design of mitochondria-targeted pyruvate dehydrogenase kinase 1 inhibitors with improved selectivity and antiproliferative activity.
Xu B, Yu Z, Xiang S, Li Y, Zhang SL, He Y.
Eur J Med Chem (2018) 155 : 275 -284
PubMed 29890389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.96 6.68
Activity 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293270 2 6.68
CHEMBL4278133 2 6.07
CHEMBL4278526 2 6.06
CHEMBL4286048 2 6.06
CHEMBL4289177 2 6.04
CHEMBL4291759 2 5.65
CHEMBL3560171 1 5.17
CHEMBL1970728 1 -
CHEMBL4289887 1 -
CHEMBL3250674 1 -
CHEMBL4286465 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293270 IC50 = 210.0 nM 6.68
CHEMBL4278133 IC50 = 850.0 nM 6.07
CHEMBL4278526 IC50 = 870.0 nM 6.06
CHEMBL4286048 IC50 = 880.0 nM 6.06
CHEMBL4289177 IC50 = 920.0 nM 6.04
CHEMBL4291759 IC50 = 2250.0 nM 5.65
CHEMBL3560171 IC50 = 6800.0 nM 5.17
CHEMBL4291759 Activity - -
CHEMBL4286465 IC50 - -
CHEMBL3250674 IC50 - -
CHEMBL4289887 IC50 - -
CHEMBL1970728 IC50 - -
CHEMBL4293270 Activity - -
CHEMBL4289177 Activity - -
CHEMBL4286048 Activity - -
CHEMBL4278526 Activity - -
CHEMBL4278133 Activity - -