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Assay Detail

CHEMBL1781772

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

Functional
Cytotoxicity against human KARPAS299 cells expressing NPM-ALK after 96 hrs by cell counting kit-8 assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KARPAS-299
Confidence 1 — Organism
Curated By Autocuration

Target

KARPAS-299 (CHEMBL2366156)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Kinoshita K, Ono Y, Emura T, Asoh K, Furuichi N, Ito T, Kawada H, Tanaka S, Morikami K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N.
Bioorg Med Chem Lett (2011) 21 : 3788 -3793
PubMed 21561771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.74 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779202 1 7.67
CHEMBL1779200 1 7.47
CHEMBL1779201 1 7.32
CHEMBL1779192 1 7.22
CHEMBL1779193 1 7.06
CHEMBL1779198 1 6.94
CHEMBL1779197 1 6.87
CHEMBL1779199 1 6.58
CHEMBL1779196 1 6.48
CHEMBL1779194 1 6.40
CHEMBL1779191 1 6.31
CHEMBL1779190 1 6.24
CHEMBL1779189 1 6.17
CHEMBL1779195 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779202 IC50 = 21.4 nM 7.67
CHEMBL1779200 IC50 = 33.6 nM 7.47
CHEMBL1779201 IC50 = 47.9 nM 7.32
CHEMBL1779192 IC50 = 60.0 nM 7.22
CHEMBL1779193 IC50 = 87.5 nM 7.06
CHEMBL1779198 IC50 = 115.0 nM 6.94
CHEMBL1779197 IC50 = 134.0 nM 6.87
CHEMBL1779199 IC50 = 263.0 nM 6.58
CHEMBL1779196 IC50 = 331.0 nM 6.48
CHEMBL1779194 IC50 = 397.0 nM 6.40
CHEMBL1779191 IC50 = 490.0 nM 6.31
CHEMBL1779190 IC50 = 570.0 nM 6.24
CHEMBL1779189 IC50 = 680.0 nM 6.17
CHEMBL1779195 IC50 = 2306.0 nM 5.64