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Assay Detail

CHEMBL4050605

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

Functional
Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562/A02
Confidence 1 — Organism
Curated By Autocuration

Target

K562/A02 (CHEMBL4296448)
Type CELL-LINE
Organism Homo sapiens

Publication

Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance.
Qiu Q, Shi W, Li Z, Zhang B, Pan M, Cui J, Dai Y, Huang W, Qian H.
J Med Chem (2017) 60 : 2930 -2943
PubMed 28301155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 4.35 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3186534 RIVOCERANIB 3.0 1 4.70
CHEMBL248976 1 4.55
CHEMBL4066132 1 4.55
CHEMBL248978 1 4.54
CHEMBL6966 VERAPAMIL 4.0 1 4.50
CHEMBL359744 DOXORUBICIN HYDROCHLORIDE 4.0 1 4.27
CHEMBL4097071 1 4.13
CHEMBL4077203 1 4.08
CHEMBL4100370 1 4.07
CHEMBL4093402 1 4.07
CHEMBL4083907 1 -
CHEMBL4073532 1 -
CHEMBL4101424 1 -
CHEMBL4104472 1 -
CHEMBL4074739 1 -
CHEMBL4066822 1 -
CHEMBL4094326 1 -
CHEMBL4077805 1 -
CHEMBL4102066 1 -
CHEMBL4085660 1 -
CHEMBL4062182 1 -
CHEMBL4091675 1 -
CHEMBL4070798 1 -
CHEMBL4099415 1 -
CHEMBL400102 1 -
CHEMBL4061101 1 -
CHEMBL4089265 1 -
CHEMBL4089366 1 -
CHEMBL4085007 1 -
CHEMBL4061215 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3186534 RIVOCERANIB IC50 = 19760.0 nM 4.70
CHEMBL248976 IC50 = 27930.0 nM 4.55
CHEMBL4066132 IC50 = 27930.0 nM 4.55
CHEMBL248978 IC50 = 28690.0 nM 4.54
CHEMBL6966 VERAPAMIL IC50 = 31280.0 nM 4.50
CHEMBL359744 DOXORUBICIN HYDROCHLORIDE IC50 = 53950.0 nM 4.27
CHEMBL4097071 IC50 = 74890.0 nM 4.13
CHEMBL4077203 IC50 = 82150.0 nM 4.08
CHEMBL4100370 IC50 = 85730.0 nM 4.07
CHEMBL4093402 IC50 = 86030.0 nM 4.07
CHEMBL4104472 IC50 > 100000.0 nM -
CHEMBL4093705 IC50 > 100000.0 nM -
CHEMBL4074739 IC50 > 100000.0 nM -
CHEMBL4066822 IC50 > 100000.0 nM -
CHEMBL4094326 IC50 > 100000.0 nM -
CHEMBL4077805 IC50 > 100000.0 nM -
CHEMBL4102066 IC50 > 100000.0 nM -
CHEMBL4085660 IC50 > 100000.0 nM -
CHEMBL4064088 IC50 > 100000.0 nM -
CHEMBL4098031 IC50 > 100000.0 nM -
CHEMBL4070940 IC50 > 100000.0 nM -
CHEMBL4068093 IC50 > 100000.0 nM -
CHEMBL4103885 IC50 > 100000.0 nM -
CHEMBL4101424 IC50 > 100000.0 nM -
CHEMBL4073532 IC50 > 100000.0 nM -
CHEMBL4083907 IC50 > 100000.0 nM -
CHEMBL4062182 IC50 > 100000.0 nM -
CHEMBL4091675 IC50 > 100000.0 nM -
CHEMBL4070798 IC50 > 100000.0 nM -
CHEMBL4099415 IC50 > 100000.0 nM -
CHEMBL400102 IC50 > 100000.0 nM -
CHEMBL4061101 IC50 > 100000.0 nM -
CHEMBL4089265 IC50 > 100000.0 nM -
CHEMBL4089366 IC50 > 100000.0 nM -
CHEMBL4085007 IC50 > 100000.0 nM -
CHEMBL4061215 IC50 > 100000.0 nM -