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Assay Detail

CHEMBL4701482

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

Functional
Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type L5178Y
Confidence 1 — Organism
Curated By Autocuration

Target

L5178Y (CHEMBL614720)
Type CELL-LINE
Organism Mus musculus

Publication

N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H receptor and cancer resistance proteins.
Szczepańska K,Kincses A,Vincze K,Szymańska E,Latacz G,Kuder KJ,Stark H,Spengler G,Handzlik J,Kieć-Kononowicz K
Bioorg Med Chem Lett (2020) 30 : 127522 -127522
PubMed 32871268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.56 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479 THIORIDAZINE 4.0 1 8.13
CHEMBL4171151 1 8.12
CHEMBL4170350 1 7.98
CHEMBL4170784 1 7.89
CHEMBL4163913 1 7.78
CHEMBL4166945 1 7.75
CHEMBL4159046 1 7.56
CHEMBL4162840 1 7.49
CHEMBL4473431 1 7.36
CHEMBL4452580 1 7.33
CHEMBL6966 VERAPAMIL 4.0 1 7.32
CHEMBL4166262 1 7.31
CHEMBL4581913 1 7.30
CHEMBL4453108 1 7.26
CHEMBL4445569 1 7.22
CHEMBL4467220 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479 THIORIDAZINE IC50 = 7.43 nM 8.13
CHEMBL4171151 IC50 = 7.59 nM 8.12
CHEMBL4170350 IC50 = 10.49 nM 7.98
CHEMBL4170784 IC50 = 12.79 nM 7.89
CHEMBL4163913 IC50 = 16.68 nM 7.78
CHEMBL4166945 IC50 = 17.6 nM 7.75
CHEMBL4159046 IC50 = 27.6 nM 7.56
CHEMBL4162840 IC50 = 32.1 nM 7.49
CHEMBL4473431 IC50 = 43.99 nM 7.36
CHEMBL4452580 IC50 = 46.23 nM 7.33
CHEMBL6966 VERAPAMIL IC50 = 47.85 nM 7.32
CHEMBL4166262 IC50 = 49.4 nM 7.31
CHEMBL4581913 IC50 = 49.7 nM 7.30
CHEMBL4453108 IC50 = 54.6 nM 7.26
CHEMBL4445569 IC50 = 60.3 nM 7.22
CHEMBL4467220 IC50 = 63.86 nM 7.20