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Assay Detail

CHEMBL3380401

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

Functional
Antileukemic activity against human SR cells assessed as inhibition of tumor growth after 24 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SR
Confidence 1 — Organism
Curated By Autocuration

Target

SR (CHEMBL614300)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel 3,5-bis(arylidene)-4-oxo-1-piperidinyl dimers: structure-activity relationships and potent antileukemic and antilymphoma cytotoxicity.
Santiago-Vazquez Y, Das S, Das U, Robles-Escajeda E, Ortega NM, Lema C, Varela-Ramírez A, Aguilera RJ, Balzarini J, De Clercq E, Dimmock SG, Gorecki DK, Dimmock JR.
Eur J Med Chem (2014) 77 : 315 -322
PubMed 24657568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.92 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391214 1 8.00
CHEMBL2391219 1 8.00
CHEMBL2012925 1 7.70
CHEMBL2391205 1 7.70
CHEMBL3313947 1 7.70
CHEMBL2391212 1 7.52
CHEMBL2391222 1 7.40
CHEMBL2391213 1 7.30
CHEMBL2391207 1 6.80
CHEMBL2391221 1 6.34
CHEMBL2391206 1 5.75
CHEMBL852 MELPHALAN 4.0 1 5.49
CHEMBL185 FLUOROURACIL 4.0 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391214 IC50 = 10.0 nM 8.00
CHEMBL2391219 IC50 = 10.0 nM 8.00
CHEMBL2012925 IC50 = 20.0 nM 7.70
CHEMBL2391205 IC50 = 20.0 nM 7.70
CHEMBL3313947 IC50 = 20.0 nM 7.70
CHEMBL2391212 IC50 = 30.0 nM 7.52
CHEMBL2391222 IC50 = 40.0 nM 7.40
CHEMBL2391213 IC50 = 50.0 nM 7.30
CHEMBL2391207 IC50 = 160.0 nM 6.80
CHEMBL2391221 IC50 = 460.0 nM 6.34
CHEMBL2391206 IC50 = 1780.0 nM 5.75
CHEMBL852 MELPHALAN IC50 = 3240.0 nM 5.49
CHEMBL185 FLUOROURACIL IC50 = 60300.0 nM 4.22