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Assay Detail

CHEMBL4268852

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Functional
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1975
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H1975 (CHEMBL614348)
Type CELL-LINE
Organism Homo sapiens

Publication

Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships.
Zhang SL, Yang Z, Hu X, Tam KY.
Bioorg Med Chem Lett (2018) 28 : 3441 -3445
PubMed 30266541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.76 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293461 1 6.70
CHEMBL4278654 1 5.90
CHEMBL4282023 1 5.80
CHEMBL4288385 1 5.76
CHEMBL4289029 1 5.70
CHEMBL4277703 1 5.70
CHEMBL4290932 1 5.70
CHEMBL4283071 1 5.70
CHEMBL4288566 1 5.70
CHEMBL4277916 1 5.70
CHEMBL4281599 1 5.70
CHEMBL3560171 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293461 IC50 = 200.0 nM 6.70
CHEMBL4278654 IC50 = 1260.0 nM 5.90
CHEMBL4282023 IC50 = 1590.0 nM 5.80
CHEMBL4288385 IC50 = 1750.0 nM 5.76
CHEMBL4289029 IC50 = 2000.0 nM 5.70
CHEMBL4277703 IC50 = 2000.0 nM 5.70
CHEMBL4290932 IC50 = 2000.0 nM 5.70
CHEMBL4283071 IC50 = 2000.0 nM 5.70
CHEMBL4288566 IC50 = 2000.0 nM 5.70
CHEMBL4277916 IC50 = 2000.0 nM 5.70
CHEMBL4281599 IC50 = 2000.0 nM 5.70
CHEMBL3560171 IC50 = 7900.0 nM 5.10