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Assay Detail

CHEMBL4605826

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

ADMET
Cytotoxicity against human LC2/ad cells assessed as reduction in cell viability incubated for 6 days by CellTiter Glo assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type LC-2-ad
Confidence 1 — Organism
Curated By Autocuration

Target

LC-2-ad (CHEMBL2366260)
Type CELL-LINE
Organism Homo sapiens

Publication

Efficacy and Tolerability of Pyrazolo[1,5-<i>a</i>]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma.
Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE.
ACS Med Chem Lett (2020) 11 : 558 -565
PubMed 32292564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.61 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4643578 1 5.89
CHEMBL4644274 1 5.82
CHEMBL4640601 1 5.80
CHEMBL4640989 1 5.57
CHEMBL4642409 1 5.55
CHEMBL4639022 1 5.55
CHEMBL4636056 1 5.47
CHEMBL4638840 1 5.26
CHEMBL4636800 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4643578 IC50 = 1300.0 nM 5.89
CHEMBL4644274 IC50 = 1500.0 nM 5.82
CHEMBL4640601 IC50 = 1600.0 nM 5.80
CHEMBL4640989 IC50 = 2700.0 nM 5.57
CHEMBL4642409 IC50 = 2800.0 nM 5.55
CHEMBL4639022 IC50 = 2800.0 nM 5.55
CHEMBL4636056 IC50 = 3400.0 nM 5.47
CHEMBL4638840 IC50 = 5500.0 nM 5.26
CHEMBL4636800 IC50 > 10000.0 nM -