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Assay Detail

CHEMBL4770080

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

ADMET
Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type L02
Confidence 1 — Organism
Curated By Autocuration

Target

L02 (CHEMBL4296457)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR NSCLCs by the conformation constrained strategy.
Chen Y,Yang L,Qiao H,Cheng Z,Xie J,Zhou W,Huang X,Jiang Y,Yu B,Zhao W
Eur J Med Chem (2020) 199 : 112388 -112388
PubMed 32402937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.41 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786343 OLMUTINIB 4.0 1 7.58
CHEMBL4780855 1 5.50
CHEMBL4791108 1 5.36
CHEMBL4785528 1 5.28
CHEMBL4779681 1 5.25
CHEMBL4800533 1 5.17
CHEMBL939 GEFITINIB 4.0 1 5.15
CHEMBL553 ERLOTINIB 4.0 1 5.14
CHEMBL4791953 1 5.10
CHEMBL4782898 1 5.08
CHEMBL4776694 1 4.90
CHEMBL4781497 1 -
CHEMBL4794102 1 -
CHEMBL4798996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786343 OLMUTINIB IC50 = 26.0 nM 7.58
CHEMBL4780855 IC50 = 3200.0 nM 5.50
CHEMBL4791108 IC50 = 4400.0 nM 5.36
CHEMBL4785528 IC50 = 5230.0 nM 5.28
CHEMBL4779681 IC50 = 5600.0 nM 5.25
CHEMBL4800533 IC50 = 6760.0 nM 5.17
CHEMBL939 GEFITINIB IC50 = 7140.0 nM 5.15
CHEMBL553 ERLOTINIB IC50 = 7250.0 nM 5.14
CHEMBL4791953 IC50 = 7990.0 nM 5.10
CHEMBL4782898 IC50 = 8370.0 nM 5.08
CHEMBL4776694 IC50 = 12470.0 nM 4.90
CHEMBL4781497 IC50 > 50000.0 nM -
CHEMBL4794102 IC50 > 20000.0 nM -
CHEMBL4798996 IC50 > 20000.0 nM -