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Assay Detail

CHEMBL4737290

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

Functional
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
Lamie PF,El-Kalaawy AM,Abdel Latif NS,Rashed LA,Philoppes JN
Eur J Med Chem (2021) 214 : 113222 -113222
PubMed 33545637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.73 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4759405 1 8.32
CHEMBL4780210 1 8.25
CHEMBL4776857 1 8.14
CHEMBL4780562 1 7.99
CHEMBL554 LAPATINIB 4.0 1 7.92
CHEMBL4753913 1 7.89
CHEMBL4797445 1 7.89
CHEMBL4754147 1 7.86
CHEMBL4781016 1 7.85
CHEMBL4763270 1 7.83
CHEMBL4785943 1 7.82
CHEMBL4751431 1 7.74
CHEMBL4791300 1 7.58
CHEMBL4752197 1 7.55
CHEMBL4762282 1 7.42
CHEMBL4758958 1 7.33
CHEMBL4753608 1 7.28
CHEMBL4790553 1 7.16
CHEMBL4741266 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4759405 IC50 = 4.8 nM 8.32
CHEMBL4780210 IC50 = 5.6 nM 8.25
CHEMBL4776857 IC50 = 7.2 nM 8.14
CHEMBL4780562 IC50 = 10.3 nM 7.99
CHEMBL554 LAPATINIB IC50 = 12.0 nM 7.92
CHEMBL4753913 IC50 = 12.9 nM 7.89
CHEMBL4797445 IC50 = 12.9 nM 7.89
CHEMBL4754147 IC50 = 13.9 nM 7.86
CHEMBL4781016 IC50 = 14.2 nM 7.85
CHEMBL4763270 IC50 = 14.7 nM 7.83
CHEMBL4785943 IC50 = 15.0 nM 7.82
CHEMBL4751431 IC50 = 18.2 nM 7.74
CHEMBL4791300 IC50 = 26.4 nM 7.58
CHEMBL4752197 IC50 = 28.1 nM 7.55
CHEMBL4762282 IC50 = 37.7 nM 7.42
CHEMBL4758958 IC50 = 46.5 nM 7.33
CHEMBL4753608 IC50 = 52.1 nM 7.28
CHEMBL4790553 IC50 = 68.9 nM 7.16
CHEMBL4741266 IC50 = 93.6 nM 7.03