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Assay Detail

CHEMBL5140670

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

Functional
Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
37
Total Activities
37
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 Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
Ding S, Gao Z, Hu Z, Qi R, Zheng X, Dong X, Zhang M, Shen J, Long T, Zhu Y, Tian L, Song W, Liu R, Li Y, Sun J, Duan W, Liu J, Chen Y.
Eur J Med Chem (2022) 238 : 114492 -114492
PubMed 35696862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.46 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353410 OSIMERTINIB 4.0 1 7.14
CHEMBL5199169 1 6.19
CHEMBL5191292 1 6.00
CHEMBL5189183 1 5.96
CHEMBL5174047 1 5.94
CHEMBL5188618 1 5.91
CHEMBL5177394 1 5.90
CHEMBL5174257 1 5.83
CHEMBL5201846 1 5.81
CHEMBL5203821 1 5.76
CHEMBL5173534 1 5.74
CHEMBL5197356 1 5.71
CHEMBL5209075 1 5.69
CHEMBL5198685 1 5.67
CHEMBL5206298 1 5.67
CHEMBL5173855 1 5.54
CHEMBL5187781 1 5.51
CHEMBL5196254 1 5.48
CHEMBL5198181 1 5.44
CHEMBL5177772 1 5.38
CHEMBL5185772 1 5.38
CHEMBL5175316 1 5.37
CHEMBL5171169 1 5.36
CHEMBL5190854 1 5.36
CHEMBL5190280 1 5.27
CHEMBL5207791 1 5.23
CHEMBL5174232 1 5.16
CHEMBL5201897 1 5.04
CHEMBL5203877 1 4.99
CHEMBL5189039 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353410 OSIMERTINIB IC50 = 72.0 nM 7.14
CHEMBL5199169 IC50 = 650.0 nM 6.19
CHEMBL5191292 IC50 = 1010.0 nM 6.00
CHEMBL5189183 IC50 = 1090.0 nM 5.96
CHEMBL5174047 IC50 = 1160.0 nM 5.94
CHEMBL5188618 IC50 = 1220.0 nM 5.91
CHEMBL5177394 IC50 = 1250.0 nM 5.90
CHEMBL5174257 IC50 = 1470.0 nM 5.83
CHEMBL5201846 IC50 = 1560.0 nM 5.81
CHEMBL5203821 IC50 = 1750.0 nM 5.76
CHEMBL5173534 IC50 = 1820.0 nM 5.74
CHEMBL5197356 IC50 = 1970.0 nM 5.71
CHEMBL5209075 IC50 = 2050.0 nM 5.69
CHEMBL5198685 IC50 = 2130.0 nM 5.67
CHEMBL5206298 IC50 = 2120.0 nM 5.67
CHEMBL5173855 IC50 = 2880.0 nM 5.54
CHEMBL5187781 IC50 = 3120.0 nM 5.51
CHEMBL5196254 IC50 = 3320.0 nM 5.48
CHEMBL5198181 IC50 = 3660.0 nM 5.44
CHEMBL5185772 IC50 = 4200.0 nM 5.38
CHEMBL5177772 IC50 = 4120.0 nM 5.38
CHEMBL5175316 IC50 = 4230.0 nM 5.37
CHEMBL5171169 IC50 = 4370.0 nM 5.36
CHEMBL5190854 IC50 = 4330.0 nM 5.36
CHEMBL5190280 IC50 = 5400.0 nM 5.27
CHEMBL5207791 IC50 = 5920.0 nM 5.23
CHEMBL5174232 IC50 = 6860.0 nM 5.16
CHEMBL5201897 IC50 = 9200.0 nM 5.04
CHEMBL5203877 IC50 = 10350.0 nM 4.99
CHEMBL5189039 IC50 = 10570.0 nM 4.98
CHEMBL5180848 IC50 = 11970.0 nM 4.92
CHEMBL5179050 IC50 = 12090.0 nM 4.92
CHEMBL5187725 IC50 = 13490.0 nM 4.87
CHEMBL5181628 IC50 = 16340.0 nM 4.79
CHEMBL5207538 IC50 = 16460.0 nM 4.78
CHEMBL5180788 IC50 = 16790.0 nM 4.78
CHEMBL5190123 IC50 = 24820.0 nM 4.61