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Assay Detail

CHEMBL5256388

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Functional
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance.
Fang L, Chu M, Yan C, Liu Y, Zhao Z.
Bioorg Med Chem (2023) 84 : 117263 -117263
PubMed 37011445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.96 5.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5277376 1 5.81
CHEMBL189963 PALBOCICLIB 4.0 1 5.09
CHEMBL5277470 1 5.02
CHEMBL4860767 1 5.01
CHEMBL5276111 1 4.93
CHEMBL5286400 1 4.92
CHEMBL5274218 1 4.89
CHEMBL5274970 1 4.84
CHEMBL5284637 1 4.84
CHEMBL5289427 1 4.79
CHEMBL5277790 1 4.78
CHEMBL5268119 1 4.76
CHEMBL5290411 1 4.75
CHEMBL5273996 1 -
CHEMBL5282077 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5277376 IC50 = 1550.0 nM 5.81
CHEMBL189963 PALBOCICLIB IC50 = 8070.0 nM 5.09
CHEMBL5277470 IC50 = 9570.0 nM 5.02
CHEMBL4860767 IC50 = 9750.0 nM 5.01
CHEMBL5276111 IC50 = 11840.0 nM 4.93
CHEMBL5286400 IC50 = 12120.0 nM 4.92
CHEMBL5274218 IC50 = 13010.0 nM 4.89
CHEMBL5274970 IC50 = 14420.0 nM 4.84
CHEMBL5284637 IC50 = 14420.0 nM 4.84
CHEMBL5289427 IC50 = 16080.0 nM 4.79
CHEMBL5277790 IC50 = 16480.0 nM 4.78
CHEMBL5268119 IC50 = 17340.0 nM 4.76
CHEMBL5290411 IC50 = 17640.0 nM 4.75
CHEMBL5273996 IC50 > 20000.0 nM -
CHEMBL5282077 IC50 > 20000.0 nM -